Ligand source activities (1 row/activity)





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DOI

1153 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
12668023 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026874 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026875 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
3341 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
6603851 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
933 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
939 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
985 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1160786 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1161520 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL588 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
DB00800 8409 58 None 6 12 Human 9.7 pAC50 = 9.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
2407 10145 76 None -7 17 Human 9.0 pAC50 = 9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 10145 76 None -7 17 Human 9.0 pAC50 = 9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 10145 76 None -7 17 Human 9.0 pAC50 = 9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 10145 76 None -7 17 Human 9.0 pAC50 = 9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 10145 76 None -7 17 Human 9.0 pAC50 = 9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
138 9855 88 None -6 10 Human 8.0 pAC50 = 8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1038/s41467-023-40064-9
1882 9855 88 None -6 10 Human 8.0 pAC50 = 8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1038/s41467-023-40064-9
5280723 9855 88 None -6 10 Human 8.0 pAC50 = 8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1038/s41467-023-40064-9
CHEMBL495 9855 88 None -6 10 Human 8.0 pAC50 = 8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1038/s41467-023-40064-9
DB00770 9855 88 None -6 10 Human 8.0 pAC50 = 8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1038/s41467-023-40064-9
4150 7575 39 None -154 15 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 7575 39 None -154 15 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 7575 39 None -154 15 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 7575 39 None -154 15 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 7575 39 None -154 15 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
2389 10104 118 None -257 29 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -257 29 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -257 29 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -257 29 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -257 29 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
2105 9828 37 None -61 24 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None -61 24 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None -61 24 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None -61 24 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None -61 24 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
3042 8196 35 None -457 17 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 8196 35 None -457 17 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 8196 35 None -457 17 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 8196 35 None -457 17 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 8196 35 None -457 17 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
17676 13844 29 None -77 13 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 13844 29 None -77 13 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 13844 29 None -77 13 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
11001318 84925 69 None 1 3 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 2 1 3 4.5 O=C(O)c1ccc2nc(-c3cc(Cl)cc(Cl)c3)oc2c1 10.1038/s41467-023-40064-9
CHEMBL2103837 84925 69 None 1 3 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 2 1 3 4.5 O=C(O)c1ccc2nc(-c3cc(Cl)cc(Cl)c3)oc2c1 10.1038/s41467-023-40064-9
135398737 7745 93 None -112 43 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -112 43 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -112 43 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -112 43 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -112 43 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
36811 8236 37 None -467 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 8236 37 None -467 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 8236 37 None -467 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 8236 37 None -467 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 8236 37 None -467 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
25102847 84996 93 None -6 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 84996 93 None -6 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
228 7233 28 None -14 19 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 7233 28 None -14 19 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 7233 28 None -14 19 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 7233 28 None -14 19 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 7233 28 None -14 19 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
168871 95905 14 None 1 13 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 95905 14 None 1 13 Human 7.9 pAC50 = 7.9 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
6077 157477 31 None -44 11 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 157477 31 None -44 11 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
54682461 91461 62 None -3 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 91461 62 None -3 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
55645 91145 8 None -53 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 91145 8 None -53 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
31101 7516 40 None -776 29 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None -776 29 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None -776 29 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None -776 29 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None -776 29 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
26879 44068 63 None 13 2 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 204 1 0 3 2.1 c1ccc([C@H]2CN3CCSC3=N2)cc1 10.1038/s41467-023-40064-9
CHEMBL1454 44068 63 None 13 2 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 204 1 0 3 2.1 c1ccc([C@H]2CN3CCSC3=N2)cc1 10.1038/s41467-023-40064-9
24826799 17570 104 None -50 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 17570 104 None -50 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2335 18620 22 None -36 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None -36 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None -36 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None -36 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
4066 211405 78 None -1071 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 211405 78 None -1071 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
154257 185398 67 None -77 19 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 185398 67 None -77 19 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
54454 12030 88 None -2 14 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 12030 88 None -2 14 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
60606 68334 73 None -9 8 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1771 68334 73 None -9 8 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
102 10899 48 None -295 20 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None -295 20 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None -295 20 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None -295 20 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None -295 20 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
5284537 40387 31 None 2 2 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 374 1 1 3 4.0 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)[C@@H]5C[C@@H]5[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL142130 40387 31 None 2 2 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 374 1 1 3 4.0 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)[C@@H]5C[C@@H]5[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
1201549 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 7384 24 None -10471 26 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
2136 9869 30 None -43 21 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 9869 30 None -43 21 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 9869 30 None -43 21 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 9869 30 None -43 21 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 9869 30 None -43 21 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
10184665 10763 51 None -1288 10 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 10763 51 None -1288 10 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 10763 51 None -1288 10 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 10763 51 None -1288 10 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 10763 51 None -1288 10 Human 5.7 pAC50 = 5.7 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
1209 8439 75 None -36 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 8439 75 None -36 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 8439 75 None -36 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 8439 75 None -36 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 8439 75 None -36 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
55483 211876 40 None -144 11 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL77622 211876 40 None -144 11 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
46780481 114308 20 None -251 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 114308 20 None -251 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 114308 20 None -251 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 114308 20 None -251 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
71137 85018 18 None - 1 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 470 12 2 9 2.7 CCOC(=O)Oc1ccc(CCNC(=O)[C@H](CCSC)NC(C)=O)cc1OC(=O)OCC 10.1038/s41467-023-40064-9
CHEMBL2106351 85018 18 None - 1 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 470 12 2 9 2.7 CCOC(=O)Oc1ccc(CCNC(=O)[C@H](CCSC)NC(C)=O)cc1OC(=O)OCC 10.1038/s41467-023-40064-9
104850 10103 96 None -2290 28 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 10103 96 None -2290 28 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 10103 96 None -2290 28 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 10103 96 None -2290 28 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 10103 96 None -2290 28 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
135564886 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 21265 5 None -8 25 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71496458 122342 87 None -72 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 122342 87 None -72 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
150 9287 21 None -22 17 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 9287 21 None -22 17 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 9287 21 None -22 17 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 9287 21 None -22 17 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 9287 21 None -22 17 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1960 9632 67 None -25 19 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 9632 67 None -25 19 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 9632 67 None -25 19 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 9632 67 None -25 19 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 9632 67 None -25 19 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
213046 9164 59 None -107 17 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None -107 17 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None -107 17 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None -107 17 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None -107 17 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
2146 9874 67 None -851 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None -851 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None -851 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None -851 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None -851 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL508338 195745 0 None -89 15 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL None None None None 10.1038/s41467-023-40064-9
1028 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 7079 71 None -1 19 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
135398745 9688 112 None -12 33 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -12 33 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -12 33 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -12 33 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135409453 10545 41 None -208 36 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None -208 36 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None -208 36 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
10531 8202 21 None -1949 26 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None -1949 26 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None -1949 26 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None -1949 26 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None -1949 26 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
37 7565 60 None -32 12 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 7565 60 None -32 12 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 7565 60 None -32 12 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 7565 60 None -32 12 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 7565 60 None -32 12 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
1816 9318 102 None -562 12 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 9318 102 None -562 12 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 9318 102 None -562 12 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 9318 102 None -562 12 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 9318 102 None -562 12 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
2865 10915 73 None -11 20 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -11 20 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -11 20 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -11 20 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -11 20 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
68555 109889 21 None 3 7 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 7 1 5 2.6 CNCCc1ccc(OC(=O)C(C)C)c(OC(=O)C(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL307739 109889 21 None 3 7 Human 7.4 pAC50 = 7.4 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 7 1 5 2.6 CNCCc1ccc(OC(=O)C(C)C)c(OC(=O)C(C)C)c1 10.1038/s41467-023-40064-9
214 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None -16 28 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
25382 15929 37 None -120 21 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 15929 37 None -120 21 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
49806720 66854 99 None -9 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 482 3 1 5 4.8 CCc1cc2c(cc1N1CCC(N3CCOCC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O 10.1038/s41467-023-40064-9
CHEMBL1738797 66854 99 None -9 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 482 3 1 5 4.8 CCc1cc2c(cc1N1CCC(N3CCOCC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O 10.1038/s41467-023-40064-9
5472 212597 75 None -7 16 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 212597 75 None -7 16 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 212597 75 None -7 16 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
2601 10552 33 None -45 17 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 10552 33 None -45 17 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 10552 33 None -45 17 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 10552 33 None -45 17 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 10552 33 None -45 17 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
242 7258 124 None -794 32 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -794 32 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -794 32 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -794 32 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -794 32 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
103 10925 61 None -79 22 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 10925 61 None -79 22 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 10925 61 None -79 22 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 10925 61 None -79 22 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 10925 61 None -79 22 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
3718 58811 73 None - 1 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 281 3 1 2 3.0 CC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
CHEMBL15870 58811 73 None - 1 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 281 3 1 2 3.0 CC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
1043 8363 14 None -5011 23 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
149 8363 14 None -5011 23 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
8223 8363 14 None -5011 23 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL442 8363 14 None -5011 23 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00696 8363 14 None -5011 23 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
1353 8692 93 None -26 39 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -26 39 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -26 39 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -26 39 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -26 39 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2220 9908 82 None -234 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 9908 82 None -234 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 9908 82 None -234 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 9908 82 None -234 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 9908 82 None -234 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2337 10030 77 None -66 29 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -66 29 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -66 29 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -66 29 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -66 29 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5852 9395 55 None -91 6 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
9931891 9395 55 None -91 6 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL239226 9395 55 None -91 6 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
16363 7383 53 None -1445 21 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 7383 53 None -1445 21 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 7383 53 None -1445 21 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 7383 53 None -1445 21 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 7383 53 None -1445 21 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
1830 9368 44 None -81 11 Human 6.1 pAC50 = 6.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 9368 44 None -81 11 Human 6.1 pAC50 = 6.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 9368 44 None -81 11 Human 6.1 pAC50 = 6.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 9368 44 None -81 11 Human 6.1 pAC50 = 6.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 9368 44 None -81 11 Human 6.1 pAC50 = 6.1 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
681 8247 72 None -77 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
940 8247 72 None -77 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
947 8247 72 None -77 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL59 8247 72 None -77 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00988 8247 72 None -77 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
212 10578 47 None -41 22 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -41 22 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -41 22 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -41 22 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -41 22 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAntagonist activity at human DRD1 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
10020353 20661 18 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL1196161 20661 18 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL556024 20661 18 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
133538 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
8443 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL574558 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
146025713 178390 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 178390 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025713 178390 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 178390 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 173204 19 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 173204 19 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75202022 177589 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
CHEMBL4453318 177589 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
16219951 178839 2 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL4472022 178839 2 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
75202022 177589 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 177589 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
173871 10386 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
936 10386 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL1193571 10386 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
46869265 23029 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 23029 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
10742 10389 31 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
1225 10389 31 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL35354 10389 31 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
92044504 178506 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 178506 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
92044504 178506 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 178506 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
1241 106955 24 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL288090 106955 24 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL552611 106955 24 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
44320092 168666 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 168666 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
167715 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 9651 14 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
1242 10385 27 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
935 10385 27 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL286080 10385 27 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
10506 9302 20 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
86290953 9302 20 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
CHEMBL3421729 9302 20 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
135 176061 123 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
3702506 176061 123 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
CHEMBL441343 176061 123 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
75201961 176409 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 176409 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
75201961 176409 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 176409 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
146025701 177350 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 177350 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025701 177350 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 177350 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
44320024 113844 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315750 113844 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 182049 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
44320050 113608 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 113608 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 182049 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
146025715 182975 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 182975 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025715 182975 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 182975 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
122324 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 6993 22 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
6077 6993 22 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
CHEMBL86931 6993 22 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
122324 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
90134269 180985 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 180985 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
75201899 178695 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 178695 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
71722299 109257 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 109257 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 109257 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
44282985 127258 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 127258 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
146025707 177886 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 177886 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320256 213092 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87172 213092 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
13720688 18326 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180542 18326 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL129634 18326 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025696 176482 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 176482 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
44331742 11212 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
CHEMBL101617 11212 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
14708665 174984 1 None - 1 Rat 5.0 pEC50 = 5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL43345 174984 1 None - 1 Rat 5.0 pEC50 = 5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
146025696 176482 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 176482 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
146025707 177886 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 177886 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 173204 19 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146034919 198979 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204559 198979 3 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
146025721 178488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 178488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
10684715 167419 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL41132 167419 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
71563083 94347 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335737 94347 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
75201901 173204 19 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
CHEMBL4277264 173204 19 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
146025721 178488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 178488 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
44276535 105165 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL275379 105165 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
44417647 88936 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 88936 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 88936 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
24878061 148189 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 148189 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
146025709 181360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 181360 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145982261 173511 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4283176 173511 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
146192959 177294 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449550 177294 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
44282985 127258 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 127258 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
130442557 173852 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4289538 173852 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
146025709 181360 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 181360 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
71722297 109249 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 109249 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 109249 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
85090332 187498 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 187498 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
90134199 179021 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 179021 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
90134199 179021 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 179021 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
44320303 170746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420788 170746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442471 182863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 182863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
681 8247 72 None -77 14 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 8247 72 None -77 14 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 8247 72 None -77 14 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 8247 72 None -77 14 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 8247 72 None -77 14 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
44554468 113045 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099225 113045 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139011 113045 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025716 180744 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 180744 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276651 106516 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL284959 106516 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
85090319 187389 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 187389 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
130442534 173676 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286177 173676 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
2030130 27751 16 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 27751 16 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025716 180744 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 180744 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145988779 174058 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
CHEMBL4293356 174058 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
44320328 213007 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
CHEMBL86669 213007 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
10689581 106939 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL287931 106939 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
3106 55294 16 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
CHEMBL15564 55294 16 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
168278276 197895 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187937 197895 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146192950 182810 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
CHEMBL4590150 182810 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
168280742 197863 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 197863 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
130442471 182863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 182863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
146192960 178298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4464150 178298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320116 170887 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 170887 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
117720272 125592 3 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
CHEMBL3421730 125592 3 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
1242 10385 27 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
935 10385 27 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
CHEMBL286080 10385 27 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
146025697 182130 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 182130 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
168276676 197241 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5178743 197241 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146025697 182130 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 182130 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
130442561 173672 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286110 173672 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
161665 179364 35 None -28 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 179364 35 None -28 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
85090324 187471 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 187471 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
6603820 102549 19 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL25856 102549 19 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
146025712 182262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 182262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
10666053 107162 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289927 107162 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
146025703 178046 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 178046 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
75201901 173204 19 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146025703 178046 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 178046 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
15696481 86441 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 86441 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
146025712 182262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 182262 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
132435 137487 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL130795 137487 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL368456 137487 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025704 179127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 179127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44554818 111043 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099234 111043 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44554472 113060 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099226 113060 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139040 113060 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85090328 187814 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 187814 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090323 188701 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 188701 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
146025813 182366 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025813 182366 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90134304 173293 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4278861 173293 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
146025821 176450 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 176450 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025821 176450 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 176450 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 180001 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 180001 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 180001 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 180001 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
85090329 189461 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 189461 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
137364078 199004 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204914 199004 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
3246443 44460 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 44460 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
146025704 179127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 179127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320053 212552 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 212552 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
11938 9190 7 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192952 9190 7 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4468760 9190 7 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44287454 20000 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1191276 20000 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL542351 20000 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
146025718 181972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 181972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
117720272 125592 3 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 125592 3 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
146025718 181972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 181972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
85090333 188080 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 188080 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
76284419 190027 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 190027 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
85090325 186528 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 186528 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
75201901 173204 19 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
CHEMBL4277264 173204 19 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
10854877 148793 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL38757 148793 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10733562 153792 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL39266 153792 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
1242 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
935 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
CHEMBL286080 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
136326241 186207 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 186207 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
146192966 182095 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
CHEMBL4573538 182095 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
44319988 212858 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85552 212858 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10758745 107209 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 107209 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 107209 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44276414 104404 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL27101 104404 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
155548298 180530 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4536851 180530 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320001 212795 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 212795 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
935 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
CHEMBL286080 10385 27 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
146025729 180938 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 180938 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44276652 106270 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL283247 106270 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
146025729 180938 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 180938 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
85090322 186238 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 186238 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090321 189592 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 189592 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168294420 199289 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5209228 199289 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
6603820 102549 19 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 102549 19 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
44554820 113063 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099222 113063 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139044 113063 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025724 179043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 179043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025819 182431 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 182431 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025819 182431 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 182431 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025724 179043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 179043 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
85090334 187404 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 187404 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090331 188232 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 188232 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
12668019 17011 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL1160787 17011 8 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
44320061 112809 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313304 112809 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
14809027 113806 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 113806 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 6993 22 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
146025727 178464 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025727 178464 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 178687 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 178687 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10506 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
130442473 174116 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 174116 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 174116 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 174116 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
1153 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
12668023 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026874 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026875 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
3341 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
6603851 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
933 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
939 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
985 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1160786 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1161520 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL588 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
DB00800 8409 58 None 6 12 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
681 8247 72 None -77 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
940 8247 72 None -77 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
947 8247 72 None -77 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
CHEMBL59 8247 72 None -77 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
DB00988 8247 72 None -77 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
75201899 178695 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
CHEMBL4469983 178695 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
201536 118245 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 118245 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
201536 118245 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 118245 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
133741 205845 11 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
CHEMBL587 205845 11 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
90134211 180808 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 180808 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
71722293 109252 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 109252 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 109252 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
44554984 111040 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099231 111040 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155541775 179823 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 179823 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
137364059 197099 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5176312 197099 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
168289194 198273 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193714 198273 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
10662054 91187 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114444 91187 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219803 91187 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
90134211 180808 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 180808 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
155519631 177184 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 177184 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
145979741 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4282096 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
6917970 10463 61 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
8370 10463 61 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
CHEMBL487387 10463 61 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
44276412 104441 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL27117 104441 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44320116 170887 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 170887 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44554649 111044 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099235 111044 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44276557 106092 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL282136 106092 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
21936384 198291 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193924 198291 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
681 8247 72 None -77 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
940 8247 72 None -77 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
947 8247 72 None -77 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
CHEMBL59 8247 72 None -77 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
DB00988 8247 72 None -77 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
15696482 86334 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2114209 86334 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
85090326 189552 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 189552 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
44320218 213203 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
CHEMBL87897 213203 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
146025811 178540 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 178540 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025811 178540 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 178540 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10640108 91186 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114441 91186 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219802 91186 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
9841398 106295 4 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL28338 106295 4 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
44320267 212991 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 212991 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10588327 20553 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1195441 20553 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL554571 20553 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
145990190 173632 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4285528 173632 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
85090337 190060 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 190060 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
21786101 162511 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
CHEMBL405519 162511 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
1241 106955 24 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL288090 106955 24 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL552611 106955 24 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
228 7233 28 None -14 19 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 7233 28 None -14 19 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 7233 28 None -14 19 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 7233 28 None -14 19 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 7233 28 None -14 19 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
155541775 179823 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 179823 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
145979741 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
CHEMBL4282096 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
145979741 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
CHEMBL4282096 173464 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
4901726 187578 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 187578 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025714 177077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 177077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025714 177077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 177077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 174116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4294397 174116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
146025730 178747 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 178747 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025730 178747 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 178747 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
9796958 153356 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 153356 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 153356 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 153356 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44320304 113812 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
CHEMBL315516 113812 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
85090318 186224 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 186224 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
10758744 107283 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL291100 107283 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
10710466 163194 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL40667 163194 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
2407 10145 76 None -7 17 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
59227 10145 76 None -7 17 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
941 10145 76 None -7 17 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL1303 10145 76 None -7 17 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
DB05271 10145 76 None -7 17 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
146192958 177293 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449549 177293 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192964 181489 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4559891 181489 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
10519435 178248 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL446350 178248 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
15981509 148736 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 148736 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
10856744 66799 11 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
CHEMBL17357 66799 11 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
85090330 187852 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 187852 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
10506 9302 20 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 9302 20 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 9302 20 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
44320050 113608 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 113608 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44320357 213178 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 213178 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86293768 125593 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421836 125593 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
228 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6604773 23030 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
CHEMBL1224528 23030 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
228 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 7233 28 None -14 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6852376 98374 13 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL1467585 98374 13 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL24077 98374 13 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL503958 98374 13 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
6603820 102549 19 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL25856 102549 19 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
145867041 181308 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4555682 181308 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
44320327 170203 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 170203 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 10385 27 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 10385 27 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 10385 27 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
137364067 197854 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187471 197854 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
10709445 108140 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 108140 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 108140 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
3033200 181306 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 181306 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
3033200 181306 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 181306 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
117720272 125592 3 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 125592 3 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
71722291 109237 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397385 109237 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040059 109237 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
146025708 180303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 180303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
25142456 89181 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
146025708 180303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 180303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276404 105854 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL28054 105854 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
10802235 20031 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1191487 20031 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL542593 20031 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
10732044 91188 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114440 91188 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219804 91188 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
75201901 173204 19 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
44554474 113062 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099227 113062 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139043 113062 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155519631 177184 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 177184 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
146025818 176541 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4438800 176541 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44320076 213205 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87910 213205 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
681 8247 72 None -77 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
940 8247 72 None -77 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
947 8247 72 None -77 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
CHEMBL59 8247 72 None -77 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
DB00988 8247 72 None -77 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
146025706 178403 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4465592 178403 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
681 8247 72 None -1380 14 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
940 8247 72 None -1380 14 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
947 8247 72 None -1380 14 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
CHEMBL59 8247 72 None -1380 14 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
DB00988 8247 72 None -1380 14 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
146025818 176541 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4438800 176541 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025706 178403 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4465592 178403 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
44555137 111041 0 None -28 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099232 111041 0 None -28 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155537335 179091 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 388 2 1 6 3.2 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1nccc2occc12 10.1021/acsmedchemlett.9b00050
CHEMBL4475239 179091 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 388 2 1 6 3.2 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1nccc2occc12 10.1021/acsmedchemlett.9b00050
681 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
940 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
947 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
CHEMBL59 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
DB00988 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
44320002 113818 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315535 113818 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44276556 106478 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL284644 106478 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
146025814 179558 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6852376 98374 13 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL1467585 98374 13 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL24077 98374 13 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL503958 98374 13 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
1242 10385 27 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 10385 27 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 10385 27 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
146025814 179558 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10540201 107005 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL288536 107005 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
681 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
940 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
947 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
CHEMBL59 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
DB00988 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
44320267 212991 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 212991 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44555138 111042 0 None -117 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099233 111042 0 None -117 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
49866139 23024 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CO2 10.1016/j.bmc.2010.07.052
CHEMBL1224452 23024 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CO2 10.1016/j.bmc.2010.07.052
1218 10388 30 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 10388 30 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 10388 30 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
44554987 111045 0 None -114 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099239 111045 0 None -114 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
13720694 19744 1 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1189465 19744 1 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL538785 19744 1 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
13720690 19862 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1190300 19862 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL540575 19862 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
155521159 177310 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 374 2 1 6 2.9 Cc1c(-c2ccc3c(c2)CCN3c2nccc3occc23)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
CHEMBL4449782 177310 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 374 2 1 6 2.9 Cc1c(-c2ccc3c(c2)CCN3c2nccc3occc23)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
6917970 10463 61 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 10463 61 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 10463 61 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
90134304 173293 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
CHEMBL4278861 173293 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
85090339 189084 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 189084 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
10518837 107249 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290842 107249 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
76284418 189097 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 189097 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090320 189342 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 189342 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
53494980 73268 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822918 73268 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852340 73268 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
10830234 107153 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289867 107153 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
681 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 8247 72 None -77 14 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
86302251 179634 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 448 4 1 5 3.5 CN(Cc1nc2cc(Br)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
CHEMBL4514994 179634 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 448 4 1 5 3.5 CN(Cc1nc2cc(Br)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
155549423 180592 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 349 3 2 7 2.3 Cc1c(-c2ccc(Nc3nccc4occc34)nc2)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
CHEMBL4538358 180592 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 349 3 2 7 2.3 Cc1c(-c2ccc(Nc3nccc4occc34)nc2)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
44320327 170203 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 170203 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
85470885 181439 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 438 4 1 5 3.8 CN(Cc1nc2cc(C(F)(F)F)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
CHEMBL4558647 181439 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 438 4 1 5 3.8 CN(Cc1nc2cc(C(F)(F)F)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
10081286 105550 2 None 1 2 Rat 5.3 pEC50 = 5.3 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effectDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
ChEMBL 192 2 3 3 0.4 NCCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
CHEMBL278188 105550 2 None 1 2 Rat 5.3 pEC50 = 5.3 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effectDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
ChEMBL 192 2 3 3 0.4 NCCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
10588326 165645 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL40950 165645 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
10831251 169952 0 None - 1 Goldfish 6.3 pEC50 = 6.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL41809 169952 0 None - 1 Goldfish 6.3 pEC50 = 6.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
13864380 213211 1 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87958 213211 1 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
13864381 215123 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL542683 215123 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL99361 215123 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
44331310 114143 1 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9502100
CHEMBL317741 114143 1 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9502100
168291403 198785 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 281 4 1 3 2.3 NS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5201584 198785 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 281 4 1 3 2.3 NS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
71563084 94346 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335736 94346 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
64638 112918 2 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 112918 2 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
6603703 6996 10 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
9637 6996 10 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
CHEMBL291143 6996 10 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
44320001 212795 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 212795 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764103 139215 13 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 139215 13 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
6453963 78314 9 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1950491 78314 9 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1962947 78314 9 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
130442590 176578 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 176578 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442590 176578 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 176578 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
44320026 212878 0 None 131 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85689 212878 0 None 131 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
117720272 125592 3 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 125592 3 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
10851849 176712 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL44414 176712 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
13720686 18332 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180562 18332 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL131313 18332 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
681 8247 72 None -1380 14 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
940 8247 72 None -1380 14 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
947 8247 72 None -1380 14 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
CHEMBL59 8247 72 None -1380 14 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
DB00988 8247 72 None -1380 14 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
146025816 176757 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025816 176757 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
9796958 153356 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 153356 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 153356 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 153356 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
228 7233 28 None -14 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
33 7233 28 None -14 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
6005 7233 28 None -14 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
CHEMBL53 7233 28 None -14 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
DB00714 7233 28 None -14 19 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
44320053 212552 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 212552 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
146025720 179727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4517022 179727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025720 179727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4517022 179727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025700 182151 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4574838 182151 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
146192953 178389 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1ccc(F)cc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4465386 178389 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1ccc(F)cc1Cl 10.1021/acsmedchemlett.9b00547
145992269 173732 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
CHEMBL4287192 173732 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
146025700 182151 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4574838 182151 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
85090335 187893 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 187893 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
6852376 98374 13 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL1467585 98374 13 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL24077 98374 13 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL503958 98374 13 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
145867041 181308 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4555682 181308 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
1153 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
12668023 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
30026874 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
30026875 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
3341 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
6603851 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
933 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
939 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
985 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL1160786 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL1161520 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL588 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
DB00800 8409 58 None -6 12 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
53494976 73374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822919 73374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852625 73374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
155560177 181709 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 378 3 1 6 2.7 Cc1nc2c(c(Oc3ccc(-c4c(C)c(=O)[nH]c(=O)n4C)c(C)c3)n1)CCC2 10.1021/acsmedchemlett.9b00050
CHEMBL4565185 181709 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 378 3 1 6 2.7 Cc1nc2c(c(Oc3ccc(-c4c(C)c(=O)[nH]c(=O)n4C)c(C)c3)n1)CCC2 10.1021/acsmedchemlett.9b00050
53494978 73276 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822920 73276 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852349 73276 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
44320129 174673 0 None 56 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL431220 174673 0 None 56 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44319976 113740 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
CHEMBL315005 113740 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
44320378 212842 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85409 212842 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10015860 106053 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL281932 106053 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
12170 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
137364063 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
CHEMBL5172089 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
146025699 177266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4449153 177266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025710 176895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4443737 176895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025699 177266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4449153 177266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
155534541 178752 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 380 4 2 6 2.5 CC(=O)Nc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 10.1021/acsmedchemlett.9b00050
CHEMBL4470808 178752 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 380 4 2 6 2.5 CC(=O)Nc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 10.1021/acsmedchemlett.9b00050
146025710 176895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4443737 176895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
10506 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
44276405 106885 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
CHEMBL287513 106885 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
130442514 173311 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4279267 173311 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
10666423 169081 0 None - 1 Goldfish 6.2 pEC50 = 6.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 363 1 3 4 4.7 Cc1cccc(-c2cc3c(s2)CN[C@H]2CCc4cc(O)c(O)cc4[C@H]32)c1 10.1021/jm970038v
CHEMBL416435 169081 0 None - 1 Goldfish 6.2 pEC50 = 6.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 363 1 3 4 4.7 Cc1cccc(-c2cc3c(s2)CN[C@H]2CCc4cc(O)c(O)cc4[C@H]32)c1 10.1021/jm970038v
146025719 177986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4459395 177986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025719 177986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4459395 177986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44319915 212744 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84557 212744 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
146025726 177546 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4452764 177546 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025823 176356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 176356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
1242 10385 27 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
935 10385 27 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
CHEMBL286080 10385 27 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
146025823 176356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 176356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
146025726 177546 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4452764 177546 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44320123 113860 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL315849 113860 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
15696487 170578 1 None 97 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420604 170578 1 None 97 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10758745 107209 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 107209 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 107209 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
14809027 113806 0 None -3 3 Rat 8.2 pEC50 = 8.2 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 113806 0 None -3 3 Rat 8.2 pEC50 = 8.2 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
6603820 102549 19 None 1 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2011.07.057
CHEMBL25856 102549 19 None 1 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2011.07.057
146025728 182792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4589664 182792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025728 182792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4589664 182792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
6604005 163896 2 None 1 4 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm9502100
CHEMBL407489 163896 2 None 1 4 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm9502100
133642 178730 10 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 178730 10 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
133642 178730 10 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 178730 10 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
44554986 113061 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099236 113061 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139041 113061 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
71722301 109250 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3040157 109250 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3216146 109250 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
130442508 177862 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
CHEMBL4457399 177862 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
71563082 94056 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2331599 94056 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
86293768 125593 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
CHEMBL3421836 125593 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
10664137 169534 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL417164 169534 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
130442508 177862 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
CHEMBL4457399 177862 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
146025725 178328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4464545 178328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025725 178328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4464545 178328 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
71722295 109244 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397381 109244 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040115 109244 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
10546132 168034 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL41196 168034 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
146025711 179811 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4518891 179811 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025711 179811 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4518891 179811 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
71562964 94350 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335740 94350 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
6603703 6996 10 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
9637 6996 10 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
CHEMBL291143 6996 10 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
64638 112918 2 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 112918 2 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44276551 104151 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL26965 104151 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276552 106656 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL285924 106656 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10497993 175253 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL43514 175253 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
44276572 103423 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL26365 103423 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
75201961 176409 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
CHEMBL4437012 176409 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
146192955 178305 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 409 4 1 4 3.8 C[C@H]1c2cccc(-c3cnn(C)c3)c2C[C@H](CO)N1C(=O)Cc1ccccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4464215 178305 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 409 4 1 4 3.8 C[C@H]1c2cccc(-c3cnn(C)c3)c2C[C@H](CO)N1C(=O)Cc1ccccc1Cl 10.1021/acsmedchemlett.9b00547
10519436 17998 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1178784 17998 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL41238 17998 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
118445551 174094 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
CHEMBL4294009 174094 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
13851595 181284 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3098131 181284 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL455497 181284 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85090338 187540 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 187540 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
14809026 212566 3 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL83080 212566 3 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
14809026 212566 3 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL83080 212566 3 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10684714 107086 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 107086 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 107086 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
146025817 182796 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 182796 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6603820 102549 19 None -6 7 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL25856 102549 19 None -6 7 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
10592479 107041 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL288846 107041 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
146025705 177393 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4450916 177393 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44554982 111039 0 None -58 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099230 111039 0 None -58 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44320257 212954 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86325 212954 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
146025705 177393 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4450916 177393 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
90142280 174075 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4293757 174075 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
9841398 106295 4 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL28338 106295 4 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10546131 107185 0 None - 1 Goldfish 7.0 pEC50 = 7.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290149 107185 0 None - 1 Goldfish 7.0 pEC50 = 7.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
6852376 98374 13 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL1467585 98374 13 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL24077 98374 13 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL503958 98374 13 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
155558060 181463 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 414 4 1 6 3.0 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1ncccc1OC(F)F 10.1021/acsmedchemlett.9b00050
CHEMBL4559240 181463 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 414 4 1 6 3.0 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1ncccc1OC(F)F 10.1021/acsmedchemlett.9b00050
146025822 180570 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4537900 180570 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025822 180570 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4537900 180570 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
107930 8311 26 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
3304 8311 26 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
CHEMBL298406 8311 26 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
DB12273 8311 26 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
3036864 209533 19 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1256645 209533 19 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1814790 209533 19 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL62 209533 19 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
155561845 182497 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4582377 182497 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
15061351 93254 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 367 2 0 6 3.0 COc1ccc2c(c1OC(C)=O)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL2314734 93254 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 367 2 0 6 3.0 COc1ccc2c(c1OC(C)=O)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
71453989 90303 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2 10.1021/jm1012374
CHEMBL2203622 90303 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2 10.1021/jm1012374
70682088 82843 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 82843 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
46931072 208824 1 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 208824 1 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
3246545 209253 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 209253 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 209253 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
70690500 82848 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 82848 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
155538443 179161 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4476383 179161 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
146025811 178540 0 None -416 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 178540 0 None -416 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
1353 8692 93 None -107 39 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3559 8692 93 None -107 39 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
86 8692 93 None -107 39 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
CHEMBL54 8692 93 None -107 39 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
DB00502 8692 93 None -107 39 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
72301 192897 76 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL487182 192897 76 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2019.04.014
44299467 204335 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
CHEMBL57029 204335 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
3246443 44460 2 None -16 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 44460 2 None -16 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
44537919 204915 0 None -60 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574700 204915 0 None -60 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
72699716 121967 0 None -12 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344459 121967 0 None -12 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
161665 179364 35 None -28 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 179364 35 None -28 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
70690498 82842 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 82842 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
13869636 108482 0 None -83 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 397 8 0 4 4.7 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1021/jm00393a037
CHEMBL299471 108482 0 None -83 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 397 8 0 4 4.7 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1021/jm00393a037
44299213 107409 0 None -77 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@@H]1C 10.1021/jm00393a037
CHEMBL292006 107409 0 None -77 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@@H]1C 10.1021/jm00393a037
44299579 204498 0 None -33 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
CHEMBL57140 204498 0 None -33 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
18367 201722 30 None -60 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 341 6 1 3 3.8 O=C(CCCN1CCC(O)(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
CHEMBL54206 201722 30 None -60 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 341 6 1 3 3.8 O=C(CCCN1CCC(O)(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
3036864 209533 19 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL1256645 209533 19 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL1814790 209533 19 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL62 209533 19 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
3036864 209533 19 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL1256645 209533 19 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL1814790 209533 19 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL62 209533 19 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
44299566 203557 0 None -67 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@H]1C 10.1021/jm00393a037
CHEMBL56547 203557 0 None -67 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@H]1C 10.1021/jm00393a037
44537925 205523 0 None -162 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 205523 0 None -162 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
129103318 174093 0 None -39 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assayAntagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 174093 0 None -39 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assayAntagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
228 7233 28 None -131 19 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
33 7233 28 None -131 19 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
6005 7233 28 None -131 19 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
CHEMBL53 7233 28 None -131 19 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
DB00714 7233 28 None -131 19 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
146025812 181670 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 181670 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025812 181670 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 181670 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90899701 176514 0 None -5 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 313 1 3 5 2.5 COc1ccc2c(c1O)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
CHEMBL4438471 176514 0 None -5 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 313 1 3 5 2.5 COc1ccc2c(c1O)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
453215 93256 8 None 7 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)C1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL2314745 93256 8 None 7 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)C1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2019.04.014
3246545 209253 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 209253 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 209253 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
146025813 182366 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025813 182366 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
3036864 209533 19 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 209533 19 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 209533 19 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 209533 19 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
1353 8692 93 None -107 39 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3559 8692 93 None -107 39 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
86 8692 93 None -107 39 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
CHEMBL54 8692 93 None -107 39 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
DB00502 8692 93 None -107 39 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3036864 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
3036864 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 209533 19 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
72699817 121966 0 None 1 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344458 121966 0 None 1 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
5018 10322 13 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
943 10322 13 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
946 10322 13 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
CHEMBL13668 10322 13 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
12269810 93257 8 None -15 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 327 2 2 5 2.8 COc1ccc2c(c1OC)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
CHEMBL2314747 93257 8 None -15 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 327 2 2 5 2.8 COc1ccc2c(c1OC)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
24837531 181553 1 None -4 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 311 2 1 4 3.1 COc1cc2c(cc1OC)C1Cc3ccc(O)cc3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL4561303 181553 1 None -4 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 311 2 1 4 3.1 COc1cc2c(cc1OC)C1Cc3ccc(O)cc3CN1CC2 10.1016/j.bmc.2019.04.014
9549058 179929 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.bmc.2019.04.014
CHEMBL4521450 179929 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.bmc.2019.04.014
146025814 179558 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
155552483 180838 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 2 1 6 2.8 COc1cc2c(c(OC)c1O)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4544045 180838 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 2 1 6 2.8 COc1cc2c(c(OC)c1O)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
146025814 179558 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
13869644 204031 0 None -109 2 Rat 5.1 pIC50 = 5.1 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 325 6 0 2 4.7 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
CHEMBL56843 204031 0 None -109 2 Rat 5.1 pIC50 = 5.1 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 325 6 0 2 4.7 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
146025815 176558 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025815 176558 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
156017431 184556 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643069 184556 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
11681599 81948 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 81948 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
133538 10391 24 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
8443 10391 24 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
CHEMBL574558 10391 24 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
11558055 79927 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 79927 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 79927 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11573628 81474 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 81474 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
9992499 80161 0 None - 0 Human 6.0 pKi = 6 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 80161 0 None - 0 Human 6.0 pKi = 6 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
11716449 147993 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 147993 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
10071501 16651 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114228 16651 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
1242 10385 27 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 10385 27 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 10385 27 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
11716438 147660 1 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 147660 1 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
16090814 88356 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 88356 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11566745 81469 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 81469 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 81469 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
11558247 82197 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 82197 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
11637457 79862 1 None - 0 Human 6.7 pKi = 6.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 79862 1 None - 0 Human 6.7 pKi = 6.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
9952858 14326 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL108764 14326 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
44408818 146943 1 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 146943 1 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
11573806 82191 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 82191 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
10467946 55243 4 None - 0 Human 8.5 pKi = 8.5 Functional
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1016/j.ejmech.2022.114378
CHEMBL155596 55243 4 None - 0 Human 8.5 pKi = 8.5 Functional
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1016/j.ejmech.2022.114378
11623343 147620 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 147620 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11493746 148101 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 148101 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
16090821 88608 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 88608 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
11718008 82066 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 82066 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
137284323 191632 0 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4852403 191632 0 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
11536995 146333 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 146333 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
147230103 186932 0 None - 2 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 186932 0 None - 2 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
5249956 80170 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 80170 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
135398737 7745 93 None -112 43 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
38 7745 93 None -112 43 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
722 7745 93 None -112 43 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
CHEMBL42 7745 93 None -112 43 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
DB00363 7745 93 None -112 43 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
11500677 147626 1 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 147626 1 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
147200197 192493 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 317 1 1 3 4.7 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4865663 192493 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 317 1 1 3 4.7 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
11595240 146966 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 146966 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11558055 79927 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 79927 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 79927 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
4350931 176092 44 None - 1 Human 7.2 pKi = 7.2 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 176092 44 None - 1 Human 7.2 pKi = 7.2 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 176092 44 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 176092 44 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
11522339 82027 1 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 82027 1 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
5249952 80183 7 None - 0 Human 6.1 pKi = 6.1 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
CHEMBL201584 80183 7 None - 0 Human 6.1 pKi = 6.1 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
135409468 8816 69 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 8816 69 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 8816 69 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
164623328 192655 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 331 2 1 3 5.0 CCc1ccc2c(c1)C(C1=CCN(C)CC1)=Nc1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4868181 192655 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 331 2 1 3 5.0 CCc1ccc2c(c1)C(C1=CCN(C)CC1)=Nc1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
149505732 193010 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4873426 193010 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
1225 8253 26 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 8253 26 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 8253 26 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 8253 26 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 8253 26 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
133538 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
8443 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
CHEMBL574558 10391 24 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
12170 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
137364063 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
CHEMBL5172089 10682 10 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
10506 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
86290953 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
CHEMBL3421729 9302 20 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
10506 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
86290953 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
CHEMBL3421729 9302 20 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
122324 6993 22 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
6077 6993 22 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
CHEMBL86931 6993 22 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
11938 9190 7 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
146192952 9190 7 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
CHEMBL4468760 9190 7 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
100 10577 58 None -7 38 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -7 38 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -7 38 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -7 38 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -7 38 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None




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3294 8787 111 None -56 44 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -56 44 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -56 44 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -56 44 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -56 44 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
103 10925 61 None -28 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 10925 61 None -28 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 10925 61 None -28 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 10925 61 None -28 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 10925 61 None -28 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
46780481 114308 20 None -29 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 114308 20 None -29 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 114308 20 None -29 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 114308 20 None -29 53 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
17676 13844 29 None - 3 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 13844 29 None - 3 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 13844 29 None - 3 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2105 9828 37 None -123 32 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None -123 32 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None -123 32 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None -123 32 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None -123 32 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL508338 195745 0 None - 6 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
6237 93579 46 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 518 3 1 3 5.1 CCc1oc2ccccc2c1C(=O)c1cc(I)c(O)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL232201 93579 46 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 518 3 1 3 5.1 CCc1oc2ccccc2c1C(=O)c1cc(I)c(O)c(I)c1 10.1038/s41467-023-40064-9
2237 9936 79 None - 3 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
3634 9936 79 None - 3 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
4887 9936 79 None - 3 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
CHEMBL21333 9936 79 None - 3 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
DB01411 9936 79 None - 3 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
60663 182448 42 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1421212 182448 42 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1534525 182448 42 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL45816 182448 42 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
1613 9127 53 None -5 44 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 9127 53 None -5 44 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 9127 53 None -5 44 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 9127 53 None -5 44 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 9127 53 None -5 44 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2993 121470 24 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL121663 121470 24 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL333826 121470 24 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
7099 202301 59 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 209 0 2 3 2.6 Nc1ccc2cc3ccc(N)cc3nc2c1 10.1038/s41467-023-40064-9
CHEMBL55400 202301 59 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 209 0 2 3 2.6 Nc1ccc2cc3ccc(N)cc3nc2c1 10.1038/s41467-023-40064-9
4151 10379 89 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 10379 89 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 10379 89 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 10379 89 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 10379 89 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
2284 9956 33 None -36 29 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 9956 33 None -36 29 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 9956 33 None -36 29 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 9956 33 None -36 29 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 9956 33 None -36 29 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
1830 9368 44 None - 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 9368 44 None - 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 9368 44 None - 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 9368 44 None - 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 9368 44 None - 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
2520 210787 70 None - 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 210787 70 None - 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 210787 70 None - 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
2865 10915 73 None -114 53 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -114 53 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -114 53 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -114 53 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -114 53 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
5354 162435 21 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL404849 162435 21 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
82146 11302 113 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
CHEMBL1023 11302 113 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
27901 84982 22 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL2105458 84982 22 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
7019 174755 106 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1308088 174755 106 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43184 174755 106 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
133 9274 52 None -30 43 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
1723 9274 52 None -30 43 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
28693 9274 52 None -30 43 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
CHEMBL19215 9274 52 None -30 43 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
DB13520 9274 52 None -30 43 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
213046 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
1577 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
2537 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5355 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5501 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
643497 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
688272 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
958 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
960 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL196677 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL26 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL267044 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB00391 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB16021 10475 110 None -537 20 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
3652 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
57 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
CHEMBL21536 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
DB15357 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
72287 67835 38 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1764 67835 38 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
237 211644 48 None - 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL546257 211644 48 None - 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL554190 211644 48 None - 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL7568 211644 48 None - 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
1027 8357 73 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3241 8357 73 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
7176 8357 73 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL1106 8357 73 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB00751 8357 73 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3055 8215 44 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
313 8215 44 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
7163 8215 44 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL936 8215 44 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
DB01231 8215 44 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
213 10625 55 None -12 43 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 10625 55 None -12 43 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 10625 55 None -12 43 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 10625 55 None -12 43 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 10625 55 None -12 43 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2337 10030 77 None -53 62 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -53 62 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -53 62 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -53 62 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -53 62 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
2406 107180 89 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
CHEMBL290106 107180 89 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
214 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None - 30 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
9417 140290 54 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 140290 54 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 140290 54 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
47979 84985 59 None - 0 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL2105581 84985 59 None - 0 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
9429 208912 58 None - 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 208912 58 None - 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
213046 9164 59 None - 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None - 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None - 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None - 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None - 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
60860 212418 30 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL1615777 212418 30 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL818 212418 30 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
2749 7132 40 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574 7132 40 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7237 7132 40 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL829 7132 40 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01246 7132 40 None - 2 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
26987 7736 33 None -245 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 7736 33 None -245 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 7736 33 None -245 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 7736 33 None -245 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 7736 33 None -245 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
3166 176199 23 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL442444 176199 23 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
135398745 9688 112 None -26 65 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -26 65 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -26 65 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -26 65 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
2398 7741 62 None -11 29 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 7741 62 None -11 29 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 7741 62 None -11 29 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 7741 62 None -11 29 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 7741 62 None -11 29 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
9419 42696 35 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1442422 42696 35 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
6726 8063 51 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7151 8063 51 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
749 8063 51 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL648 8063 51 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB01176 8063 51 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
16960 21259 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1201287 21259 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
5584 209990 44 None - 1 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL644 209990 44 None - 1 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
9853053 127297 74 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL354541 127297 74 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
1765 10589 98 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
4184 10589 98 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
9871419 10589 98 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
CHEMBL398435 10589 98 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
DB08816 10589 98 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
54454 12030 88 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 12030 88 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
12488 8438 56 None -19 23 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
941361 8438 56 None -19 23 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
CHEMBL30008 8438 56 None -19 23 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
DB04841 8438 56 None -19 23 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
68802 116812 37 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
CHEMBL32350 116812 37 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
49843517 85069 41 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
CHEMBL2107831 85069 41 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
3606 210267 60 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL6615 210267 60 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
135 9310 43 None -91 56 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -91 56 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -91 56 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -91 56 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -91 56 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
10219 195575 37 None - 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL493439 195575 37 None - 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL50588 195575 37 None - 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
134 9292 24 None -263 67 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 9292 24 None -263 67 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 9292 24 None -263 67 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 9292 24 None -263 67 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 9292 24 None -263 67 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1890 9535 49 None - 16 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None - 16 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None - 16 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None - 16 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None - 16 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
5489013 64179 32 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 8 2 4 3.0 COc1cccc(C(=O)CCN[C@@H](C)[C@H](O)c2ccccc2)c1 10.1038/s41467-023-40064-9
CHEMBL1651913 64179 32 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 8 2 4 3.0 COc1cccc(C(=O)CCN[C@@H](C)[C@H](O)c2ccccc2)c1 10.1038/s41467-023-40064-9
115358 108339 38 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 463 9 2 6 5.9 COc1cc(C)c2c(Oc3cccc(C(F)(F)F)c3)c(OC)cc(NC(C)CCCN)c2n1 10.1038/s41467-023-40064-9
CHEMBL298470 108339 38 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 463 9 2 6 5.9 COc1cc(C)c2c(Oc3cccc(C(F)(F)F)c3)c(OC)cc(NC(C)CCCN)c2n1 10.1038/s41467-023-40064-9
1577 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
2537 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5355 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5501 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
643497 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
688272 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
958 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
960 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL196677 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL26 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL267044 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB00391 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB16021 10475 110 None -537 20 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
2162 48288 100 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 48288 100 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL508338 195745 0 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
5568 204279 29 None - 5 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
66069 204279 29 None - 5 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL1201102 204279 29 None - 5 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL570 204279 29 None - 5 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
71277 91314 27 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 789 9 4 15 2.7 CCC(=O)O[C@H]1[C@H](O[C@@H]2[C@@H](C)[C@H](O[C@H]3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@](C)(O)[C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@]2(C)O)O[C@H](C)C[C@@H]1N(C)C 10.1038/s41467-023-40064-9
CHEMBL2220427 91314 27 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 789 9 4 15 2.7 CCC(=O)O[C@H]1[C@H](O[C@@H]2[C@@H](C)[C@H](O[C@H]3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@](C)(O)[C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@]2(C)O)O[C@H](C)C[C@@H]1N(C)C 10.1038/s41467-023-40064-9
2286 9957 51 None -30 30 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 9957 51 None -30 30 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 9957 51 None -30 30 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 9957 51 None -30 30 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 9957 51 None -30 30 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
22323 22071 32 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9571037 22071 32 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1213553 22071 32 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
2146 9874 67 None - 9 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None - 9 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None - 9 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None - 9 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None - 9 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6834 212331 45 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL811 212331 45 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
191 7191 98 None -26 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 7191 98 None -26 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 7191 98 None -26 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 7191 98 None -26 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 7191 98 None -26 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
1909 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
2559 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
4474 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL1484 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL3302409 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
DB00622 9598 64 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
212 10578 47 None -6 25 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -6 25 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -6 25 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -6 25 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -6 25 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2335 18620 22 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
25025298 84926 39 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
CHEMBL2103855 84926 39 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
103 10925 61 None -28 53 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 10925 61 None -28 53 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 10925 61 None -28 53 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 10925 61 None -28 53 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 10925 61 None -28 53 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
3601 21275 9 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1201349 21275 9 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
2762 10635 31 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5587 10635 31 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
7318 10635 31 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1241 10635 31 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
DB00792 10635 31 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5583 19816 51 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 369 6 3 8 2.7 COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL119 19816 51 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 369 6 3 8 2.7 COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC 10.1038/s41467-023-40064-9
22530 62904 58 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1600878 62904 58 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1625607 62904 58 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
62867 9903 35 None - 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
7557 9903 35 None - 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL398880 9903 35 None - 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01621 9903 35 None - 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
9822750 85184 65 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL2111097 85184 65 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
25151352 147384 67 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 147384 67 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
1547484 7727 74 None - 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 7727 74 None - 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 7727 74 None - 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 7727 74 None - 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 7727 74 None - 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4167 21272 43 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL1201342 21272 43 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
40973 52809 70 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 1 1 1 4.9 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CCCC[C@@H]4[C@H]3C(=C)C[C@@]21CC 10.1038/s41467-023-40064-9
CHEMBL1533 52809 70 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 1 1 1 4.9 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CCCC[C@@H]4[C@H]3C(=C)C[C@@]21CC 10.1038/s41467-023-40064-9
4418 40996 85 None - 7 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 40996 85 None - 7 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
3344 205097 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 260 3 1 3 1.8 O=C1NCC2(CCN(CCc3ccccc3)CC2)O1 10.1038/s41467-023-40064-9
CHEMBL576127 205097 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 260 3 1 3 1.8 O=C1NCC2(CCN(CCc3ccccc3)CC2)O1 10.1038/s41467-023-40064-9
242 7258 124 None -281 51 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -281 51 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -281 51 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -281 51 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -281 51 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
9601226 109177 7 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 563 14 1 6 6.1 CCC(=O)O[C@@H](O[P@](=O)(CCCCc1ccccc1)CC(=O)N1C[C@H](C2CCCCC2)C[C@H]1C(=O)O)C(C)C 10.1038/s41467-023-40064-9
CHEMBL3039598 109177 7 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 563 14 1 6 6.1 CCC(=O)O[C@@H](O[P@](=O)(CCCCc1ccccc1)CC(=O)N1C[C@H](C2CCCCC2)C[C@H]1C(=O)O)C(C)C 10.1038/s41467-023-40064-9
138106885 173690 75 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
36314 173690 75 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
CHEMBL428647 173690 75 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
3336 101776 30 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1405922 101776 30 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL254832 101776 30 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4601 213526 35 None - 17 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201023 213526 35 None - 17 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL900 213526 35 None - 17 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
102 10899 48 None -25118 49 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None -25118 49 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None -25118 49 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None -25118 49 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None -25118 49 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
25295 20392 37 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1194287 20392 37 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
9417 140290 54 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 140290 54 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 140290 54 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
11057 182928 23 None -2 20 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
3468 182928 23 None -2 20 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL459265 182928 23 None -2 20 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL64894 182928 23 None -2 20 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
2585 7590 103 None -112 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None -112 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None -112 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None -112 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None -112 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
3117 214620 103 None -2 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
CHEMBL964 214620 103 None -2 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
1599 9120 50 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955 9120 50 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7215 9120 50 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL841 9120 50 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00836 9120 50 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
135398737 7745 93 None -44 90 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -44 90 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -44 90 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -44 90 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -44 90 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
16564 211774 32 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
CHEMBL76725 211774 32 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
4417 62336 54 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1439099 62336 54 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1620794 62336 54 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL4744444 220813 32 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1C(=O)NCC(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@H](CO)C(=O)N[C@@H]([C@H](C)CC(=O)O)C(=O)N[C@@H](CC(=O)c2ccccc2N)C(=O)O[C@@H]1C 10.1038/s41467-023-40064-9
31101 7516 40 None -436 35 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None -436 35 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None -436 35 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None -436 35 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None -436 35 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
1613 9127 53 None -5 44 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 9127 53 None -5 44 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 9127 53 None -5 44 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 9127 53 None -5 44 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 9127 53 None -5 44 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3627 50903 18 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1515447 50903 18 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
93154 12208 29 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL107360 12208 29 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
16222096 87258 67 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
CHEMBL2146883 87258 67 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
1227 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
2331 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
3957 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
4992 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL511 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
DB06691 9267 43 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
5022 8432 76 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248 8432 76 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
8182 8432 76 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL231068 8432 76 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
DB04908 8432 76 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6077 157477 31 None - 0 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 157477 31 None - 0 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
3561 25849 39 None -1 11 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL1289 25849 39 None -1 11 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
441383 27105 57 None -12 17 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1306 27105 57 None -12 17 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
259329 67278 31 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 519 7 2 4 5.3 C[C@]12CC[C@@H]3c4ccc(OC(=O)N(CCCl)CCCl)cc4CC[C@H]3[C@@H]1CC[C@@H]2OP(=O)(O)O 10.1038/s41467-023-40064-9
CHEMBL1756 67278 31 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 519 7 2 4 5.3 C[C@]12CC[C@@H]3c4ccc(OC(=O)N(CCCl)CCCl)cc4CC[C@H]3[C@@H]1CC[C@@H]2OP(=O)(O)O 10.1038/s41467-023-40064-9
2181 9902 46 None - 34 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
4830 9902 46 None - 34 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
92 9902 46 None - 34 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL440294 9902 46 None - 34 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
DB09286 9902 46 None - 34 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL5291995 201315 0 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 341 5 0 5 3.3 CN(C)CCCN1C(=O)c2cc([N+](=O)[O-])ccc2Oc2ccccc21 10.1038/s41467-023-40064-9
4098 39279 30 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1255739 39279 30 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1411979 39279 30 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
1153 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
12668023 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026874 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026875 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
3341 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
6603851 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
933 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
939 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
985 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1160786 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1161520 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL588 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
DB00800 8409 58 None -32 10 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
4485 76154 118 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL193 76154 118 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
1190 7669 47 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
25074887 7669 47 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
583 7669 47 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1200490 7669 47 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00050 7669 47 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
48041 113858 46 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
CHEMBL315838 113858 46 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
40 8329 58 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
77993 8329 58 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
995 8329 58 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1510 8329 58 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
DB00216 8329 58 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
37464 25993 26 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1290 25993 26 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
3584 10549 64 None - 14 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 10549 64 None - 14 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 10549 64 None - 14 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 10549 64 None - 14 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 10549 64 None - 14 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
3158 63041 27 None -2398 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 63041 27 None -2398 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2237 9936 79 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
3634 9936 79 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
4887 9936 79 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
CHEMBL21333 9936 79 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
DB01411 9936 79 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1038/s41467-023-40064-9
25025298 84926 39 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
CHEMBL2103855 84926 39 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
228 7233 28 None -35 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 7233 28 None -35 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 7233 28 None -35 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 7233 28 None -35 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 7233 28 None -35 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
9571107 174298 33 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 389 5 2 8 1.0 CO/N=C1\CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3C2CC2)CC1CN 10.1038/s41467-023-40064-9
CHEMBL430 174298 33 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 389 5 2 8 1.0 CO/N=C1\CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3C2CC2)CC1CN 10.1038/s41467-023-40064-9
2600 10551 74 None -7 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None -7 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None -7 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None -7 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None -7 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
150311 16584 102 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL1138 16584 102 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
2444 21250 26 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
CHEMBL1201245 21250 26 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
2799 46568 55 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 364 4 1 1 7.0 CC(C)(C)CC(C)(C)c1ccc(O)c(Cc2ccc(Cl)cc2Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1476605 46568 55 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 364 4 1 1 7.0 CC(C)(C)CC(C)(C)c1ccc(O)c(Cc2ccc(Cl)cc2Cl)c1 10.1038/s41467-023-40064-9
11154555 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
5037 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
7671 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL2028019 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL3085826 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB06016 7587 62 None -1445 12 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
11976 7707 59 None -12 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 7707 59 None -12 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 7707 59 None -12 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 7707 59 None -12 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
2865 10915 73 None -114 53 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -114 53 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -114 53 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -114 53 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -114 53 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL4743867 220812 14 None - 0 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
3158 63041 27 None -2398 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 63041 27 None -2398 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
277 8083 62 None -33 50 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913 8083 62 None -33 50 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
765 8083 62 None -33 50 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL516 8083 62 None -33 50 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB00434 8083 62 None -33 50 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
1427 8794 54 None -977 27 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 8794 54 None -977 27 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 8794 54 None -977 27 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 8794 54 None -977 27 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 8794 54 None -977 27 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
15387 52596 55 None - 24 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1531134 52596 55 None - 24 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
2286 9957 51 None -30 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 9957 51 None -30 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 9957 51 None -30 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 9957 51 None -30 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 9957 51 None -30 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
124087 8171 114 None - 15 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 8171 114 None - 15 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 8171 114 None - 15 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 8171 114 None - 15 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 8171 114 None - 15 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
2105 9828 37 None -123 32 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None -123 32 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None -123 32 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None -123 32 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None -123 32 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
9571107 174298 33 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 389 5 2 8 1.0 CO/N=C1\CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3C2CC2)CC1CN 10.1038/s41467-023-40064-9
CHEMBL430 174298 33 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 389 5 2 8 1.0 CO/N=C1\CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3C2CC2)CC1CN 10.1038/s41467-023-40064-9
3678 101567 57 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL253371 101567 57 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
2335 18620 22 None - 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None - 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None - 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None - 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
54758501 145845 58 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
CHEMBL3786343 145845 58 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
71109 84981 10 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 272 4 1 4 2.9 OC(CN1CCCCC1)c1cc(-c2ccccc2)on1 10.1038/s41467-023-40064-9
CHEMBL2105453 84981 10 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 272 4 1 4 2.9 OC(CN1CCCCC1)c1cc(-c2ccccc2)on1 10.1038/s41467-023-40064-9
1971 9641 38 None -8 30 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 9641 38 None -8 30 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 9641 38 None -8 30 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 9641 38 None -8 30 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 9641 38 None -8 30 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2389 10104 118 None -489 66 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -489 66 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -489 66 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -489 66 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -489 66 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
2771 201796 74 None -120 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 201796 74 None -120 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 201796 74 None -120 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
34040 34858 72 None - 1 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
CHEMBL1372950 34858 72 None - 1 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
2865 10915 73 None -114 53 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -114 53 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -114 53 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -114 53 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -114 53 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
2601 10552 33 None -16 21 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 10552 33 None -16 21 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 10552 33 None -16 21 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 10552 33 None -16 21 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 10552 33 None -16 21 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
12555 24733 53 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL12610 24733 53 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
11167602 77235 116 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 482 5 3 4 5.7 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1946170 77235 116 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 482 5 3 4 5.7 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1 10.1038/s41467-023-40064-9
1548955 95356 20 None - 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2800 95356 20 None - 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL2355051 95356 20 None - 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
1212 8443 50 None -51 65 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 8443 50 None -51 65 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 8443 50 None -51 65 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 8443 50 None -51 65 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 8443 50 None -51 65 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
25102847 84996 93 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 84996 93 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
1588 9105 27 None -131 44 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
28864 9105 27 None -131 44 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
43 9105 27 None -131 44 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL157138 9105 27 None -131 44 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB00589 9105 27 None -131 44 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
135398737 7745 93 None -44 90 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -44 90 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -44 90 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -44 90 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -44 90 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
180 7189 56 None -109 40 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None -109 40 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None -109 40 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None -109 40 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None -109 40 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
193962 110570 106 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 434 4 2 7 4.7 Cc1cc(C#N)cc(C)c1Oc1nc(Nc2ccc(C#N)cc2)nc(N)c1Br 10.1038/s41467-023-40064-9
CHEMBL308954 110570 106 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 434 4 2 7 4.7 Cc1cc(C#N)cc(C)c1Oc1nc(Nc2ccc(C#N)cc2)nc(N)c1Br 10.1038/s41467-023-40064-9
1353 8692 93 None -38 85 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -38 85 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -38 85 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -38 85 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -38 85 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3157 8252 71 None - 12 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 8252 71 None - 12 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 8252 71 None - 12 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 8252 71 None - 12 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 8252 71 None - 12 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
5328940 106992 107 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
135398737 7745 93 None -44 90 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -44 90 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -44 90 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -44 90 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -44 90 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
65772 67177 8 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL174984 67177 8 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
135 9310 43 None -91 56 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -91 56 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -91 56 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -91 56 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -91 56 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2683 109665 25 None - 16 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL305906 109665 25 None - 16 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL334255 109665 25 None - 16 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
16362 9899 71 None -52480 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None -52480 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None -52480 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None -52480 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None -52480 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
5351322 101566 38 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL25336 101566 38 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
65863 21237 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1201196 21237 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
115368 9830 47 None - 4 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
2112 9830 47 None - 4 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
7556 9830 47 None - 4 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1472975 9830 47 None - 4 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
DB08922 9830 47 None - 4 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
208898 72973 78 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
CHEMBL184412 72973 78 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
1086 8371 27 None - 2 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290 8371 27 None - 2 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
7181 8371 27 None - 2 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
CHEMBL1206 8371 27 None - 2 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
DB00392 8371 27 None - 2 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
2337 10030 77 None -53 62 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -53 62 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -53 62 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -53 62 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -53 62 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
2726 7706 68 None -36 72 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 7706 68 None -36 72 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 7706 68 None -36 72 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 7706 68 None -36 72 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 7706 68 None -36 72 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
448537 167029 89 None -28 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 167029 89 None -28 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
10531 8202 21 None -218 24 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None -218 24 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None -218 24 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None -218 24 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None -218 24 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
4822 51806 47 None - 1 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL152408 51806 47 None - 1 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
2407 10145 76 None -128 7 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 10145 76 None -128 7 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 10145 76 None -128 7 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 10145 76 None -128 7 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 10145 76 None -128 7 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
49843517 85069 41 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
CHEMBL2107831 85069 41 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
25151352 147384 67 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 147384 67 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay (CRO assay) measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
11167602 77235 116 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 482 5 3 4 5.7 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1946170 77235 116 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 482 5 3 4 5.7 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1 10.1038/s41467-023-40064-9
10071196 9898 79 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
5142 9898 79 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
8423 9898 79 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
CHEMBL2111101 9898 79 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
DB05316 9898 79 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
71897 85023 19 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
CHEMBL2106537 85023 19 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
2805 168669 38 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL415087 168669 38 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
114948 67071 14 None - 3 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL1743263 67071 14 None - 3 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
16351 109507 47 None - 6 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 109507 47 None - 6 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
123879 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1910 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1911 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
2354 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
CHEMBL361812 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
DB13036 10060 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
10180 105645 47 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL279014 105645 47 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
3598 194600 76 None - 7 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL496 194600 76 None - 7 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
37 7565 60 None -14 17 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 7565 60 None -14 17 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 7565 60 None -14 17 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 7565 60 None -14 17 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 7565 60 None -14 17 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
1524 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
197 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
88 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL51 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB12465 8962 96 None -79 51 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
242 7258 124 None -281 51 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -281 51 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -281 51 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -281 51 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -281 51 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
21855 91021 42 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL22108 91021 42 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
5353853 24758 47 None -19 15 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9556529 24758 47 None -19 15 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1262 24758 47 None -19 15 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
2389 10104 118 None -489 66 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -489 66 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -489 66 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -489 66 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -489 66 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
6077 157477 31 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 157477 31 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
3294 8787 111 None -56 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -56 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -56 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -56 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -56 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2710 91083 31 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL22150 91083 31 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
43082 67057 37 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1742452 67057 37 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
98941 53724 17 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL154126 53724 17 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
2107 9829 50 None -5 2 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747 9829 50 None -5 2 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
9216 9829 50 None -5 2 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL251940 9829 50 None -5 2 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB01608 9829 50 None -5 2 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5440 35497 37 None -1 9 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 35497 37 None -1 9 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
104903 63118 17 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 10.1038/s41467-023-40064-9
CHEMBL1630578 63118 17 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 10.1038/s41467-023-40064-9
1712 9270 43 None -6 22 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
4078 9270 43 None -6 22 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
7227 9270 43 None -6 22 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
CHEMBL1088 9270 43 None -6 22 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
DB00933 9270 43 None -6 22 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
2771 201796 74 None -120 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 201796 74 None -120 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 201796 74 None -120 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2446 161432 57 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 7 2 4 2.1 CCN(CC)CCNC(=O)c1cc(Br)c(N)cc1OC 10.1038/s41467-023-40064-9
CHEMBL399510 161432 57 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 343 7 2 4 2.1 CCN(CC)CCNC(=O)c1cc(Br)c(N)cc1OC 10.1038/s41467-023-40064-9
681 8247 72 None -154 38 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
940 8247 72 None -154 38 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
947 8247 72 None -154 38 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL59 8247 72 None -154 38 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00988 8247 72 None -154 38 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
3103 48432 49 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1492 48432 49 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
135398745 9688 112 None -26 65 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -26 65 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -26 65 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -26 65 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
212 10578 47 None -6 25 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -6 25 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -6 25 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -6 25 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -6 25 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
242 7258 124 None -281 51 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -281 51 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -281 51 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -281 51 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -281 51 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
3952 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5443 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL1331786 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL420 8669 38 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
2389 10104 118 None -489 66 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -489 66 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -489 66 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -489 66 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -489 66 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
129893322 35391 56 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
4923 35391 56 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353897 35391 56 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
6178111 35391 56 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1377 35391 56 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
2337 10030 77 None -53 62 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -53 62 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -53 62 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -53 62 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -53 62 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
1209 8439 75 None - 32 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 8439 75 None - 32 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 8439 75 None - 32 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 8439 75 None - 32 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 8439 75 None - 32 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
5591 164310 90 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
CHEMBL408 164310 90 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
3280 55223 28 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL1555736 55223 28 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
4209 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 9937 75 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
3053 211913 95 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 393 16 5 8 -2.7 O=C(O)CN(CCN(CC(=O)O)CC(=O)O)CCN(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL780 211913 95 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 393 16 5 8 -2.7 O=C(O)CN(CCN(CC(=O)O)CC(=O)O)CCN(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
5205 84962 58 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
CHEMBL2104895 84962 58 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
CHEMBL1630575 63117 0 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 1093 23 16 18 -3.3 CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@H]([C@H](O)CCN)NC(=O)[C@H]([C@H](O)[C@@H](O)c2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H]([C@@H](C)O)NC1=O 10.1038/s41467-023-40064-9
443869 84916 45 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2103761 84916 45 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
1353 8692 93 None -38 85 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -38 85 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -38 85 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -38 85 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -38 85 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2600 10551 74 None -7 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None -7 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None -7 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None -7 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None -7 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
180 7189 56 None -109 40 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None -109 40 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None -109 40 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None -109 40 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None -109 40 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2580 85170 18 None - 2 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL2110775 85170 18 None - 2 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
4756 23421 50 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 23421 50 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 23421 50 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
1153 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
12668023 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026874 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026875 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
3341 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
6603851 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
933 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
939 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
985 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1160786 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1161520 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL588 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
DB00800 8409 58 None -32 10 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
1353 8692 93 None -38 85 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -38 85 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -38 85 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -38 85 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -38 85 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
3783 20777 23 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 4 2.9 CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL1197051 20777 23 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 301 7 3 4 2.9 CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
6075 156887 42 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL395110 156887 42 None - 16 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
4735 201894 96 None - 10 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL361506 201894 96 None - 10 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL55 201894 96 None - 10 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
4034 62596 55 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 62596 55 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
2247 7293 81 None -61 42 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 7293 81 None -61 42 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 7293 81 None -61 42 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 7293 81 None -61 42 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 7293 81 None -61 42 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation countingBinding affinity towards human DRD1 in an in vitro assay with cellular components (NIBR assay) measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
146025821 176450 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 176450 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025821 176450 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 176450 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 182796 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 182796 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146192964 181489 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4559891 181489 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
681 8247 72 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
940 8247 72 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
947 8247 72 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
CHEMBL59 8247 72 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
DB00988 8247 72 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
6852376 98374 13 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL1467585 98374 13 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL24077 98374 13 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL503958 98374 13 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
11938 9190 7 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 9190 7 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 9190 7 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
75201901 173204 19 None -1 24 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -1 24 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442471 182863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 182863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
75201961 176409 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
CHEMBL4437012 176409 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
130442471 182863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 182863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
75201901 173204 19 None -1 24 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -1 24 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
4901726 187578 9 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 187578 9 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
12668019 17011 8 None 204 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL1160787 17011 8 None 204 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
6603820 102549 19 None -4 12 Human 7.9 pEC50 = 7.9 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 102549 19 None -4 12 Human 7.9 pEC50 = 7.9 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
146025820 180001 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 180001 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
681 8247 72 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 8247 72 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 8247 72 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 8247 72 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 8247 72 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
85090318 186224 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 186224 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
146192966 182095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acs.jmedchem.1c01887
CHEMBL4573538 182095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acs.jmedchem.1c01887
85090319 187389 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 187389 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090338 187540 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 187540 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090320 189342 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 189342 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090337 190060 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 190060 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
11938 9190 7 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 9190 7 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 9190 7 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090325 186528 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 186528 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090334 187404 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 187404 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
132016545 179855 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 333 2 0 1 4.7 C[C@H]1c2ccccc2CCN1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4519818 179855 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 333 2 0 1 4.7 C[C@H]1c2ccccc2CCN1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
9796958 153356 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL2115374 153356 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL39230 153356 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL544814 153356 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
130442473 174116 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 174116 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 174116 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 174116 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
85090335 187893 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 187893 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
85090330 187852 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 187852 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
167715 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
24133757 178379 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 340 1 1 2 5.2 CC1c2ccsc2CCN1C(=O)Nc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4465320 178379 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 340 1 1 2 5.2 CC1c2ccsc2CCN1C(=O)Nc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
167715 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 9651 14 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
133642 178730 10 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 178730 10 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
133642 178730 10 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 178730 10 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
10742 10389 31 None -2 8 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
1225 10389 31 None -2 8 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL35354 10389 31 None -2 8 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
10020353 20661 18 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL1196161 20661 18 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL556024 20661 18 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
85090328 187814 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 187814 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
146025701 177350 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 177350 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025713 178390 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 178390 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025701 177350 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 177350 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025713 178390 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 178390 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442480 182049 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
130442480 182049 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
146025816 176757 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
1242 10385 27 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
935 10385 27 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
CHEMBL286080 10385 27 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
146192967 197891 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 485 5 1 5 4.5 C[C@H]1c2cccc(-c3cnn(C4COC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL5187909 197891 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 485 5 1 5 4.5 C[C@H]1c2cccc(-c3cnn(C4COC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146025816 176757 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
130442590 176578 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 176578 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442590 176578 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 176578 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442572 178687 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 178687 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
6603703 6996 10 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
9637 6996 10 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
CHEMBL291143 6996 10 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
1153 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
12668023 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026874 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026875 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
3341 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
6603851 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
933 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
939 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
985 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1160786 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1161520 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL588 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
DB00800 8409 58 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
75201901 173204 19 None -1 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
CHEMBL4277264 173204 19 None -1 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
2030130 27751 16 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 27751 16 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090324 187471 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 187471 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
76284418 189097 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 189097 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
75202022 177589 2 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 177589 2 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
146025815 176558 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
1218 10388 30 None -11 8 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 10388 30 None -11 8 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 10388 30 None -11 8 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
146025815 176558 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
85090321 189592 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 189592 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090323 188701 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 188701 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
146266 107474 8 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL292418 107474 8 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL540857 107474 8 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
146025823 176356 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 176356 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
146025823 176356 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 176356 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
85090322 186238 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 186238 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
75201899 178695 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 178695 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
228 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
3033200 181306 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 181306 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
85090333 188080 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 188080 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090326 189552 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 189552 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
228 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 7233 28 None -35 23 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
3033200 181306 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 181306 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
85090332 187498 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 187498 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
6852376 98374 13 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL1467585 98374 13 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL24077 98374 13 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL503958 98374 13 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
146192960 178298 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4464150 178298 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090339 189084 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 189084 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
136326241 186207 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 186207 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
92044504 178506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 178506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
92044504 178506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 178506 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
3045992 182854 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 182854 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90134269 180985 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 180985 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
90134269 180985 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 180985 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
3045992 182854 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 182854 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
85090329 189461 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 189461 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090331 188232 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 188232 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
76284419 190027 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 190027 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
9841398 106295 4 None -3 4 Human 8.1 pEC50 = 8.1 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
CHEMBL28338 106295 4 None -3 4 Human 8.1 pEC50 = 8.1 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
1218 10388 30 None -11 8 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
938 10388 30 None -11 8 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL353335 10388 30 None -11 8 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
72548703 168346 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 168346 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
3036864 209533 19 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1256645 209533 19 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1814790 209533 19 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL62 209533 19 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
3036864 209533 19 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 209533 19 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 209533 19 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 209533 19 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
5281878 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
5281881 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
948 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
968 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
CHEMBL42055 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
CHEMBL54661 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
DB00875 8441 35 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
5018 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
943 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
946 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
CHEMBL13668 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
5018 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
943 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
946 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
CHEMBL13668 10322 13 None 2 10 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
44358126 33452 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 315 1 1 2 4.2 C[C@H]1N(C)CCc2cc(Cl)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm00022a004
CHEMBL136190 33452 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 315 1 1 2 4.2 C[C@H]1N(C)CCc2cc(Cl)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm00022a004
3036864 209533 19 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL1256645 209533 19 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL1814790 209533 19 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL62 209533 19 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
11795296 33540 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 33540 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL1256645 209533 19 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL1814790 209533 19 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL62 209533 19 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
10809333 33964 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 33964 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10522247 33504 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 33504 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL1256645 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL1814790 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL62 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
10784787 33494 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 360 2 0 3 5.0 CN1CCN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136226 33494 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 360 2 0 3 5.0 CN1CCN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
11795296 33540 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 33540 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL1256645 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL1814790 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL62 209533 19 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
10712649 125985 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 125985 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10810927 126074 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 126074 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
10522247 33504 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 33504 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
11794473 126108 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCC2 10.1021/jm00022a004
CHEMBL344206 126108 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCC2 10.1021/jm00022a004
10810927 126074 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 126074 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 209533 19 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 209533 19 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 209533 19 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
10787324 33629 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 402 4 1 3 4.4 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCO 10.1021/jm00022a004
CHEMBL136340 33629 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 402 4 1 3 4.4 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCO 10.1021/jm00022a004
10574585 34198 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 34198 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
3036864 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL1256645 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL1814790 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL62 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
3036864 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL1256645 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL1814790 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL62 209533 19 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
10043978 34021 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 34021 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10525990 34345 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 5 1 3 4.8 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCCO 10.1021/jm00022a004
CHEMBL136932 34345 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 5 1 3 4.8 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCCO 10.1021/jm00022a004
10247592 35677 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 35677 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
6603950 210103 9 None -6 8 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 210103 9 None -6 8 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
6603950 210103 9 None -6 8 Rat 8.9 pIC50 = 8.9 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL64875 210103 9 None -6 8 Rat 8.9 pIC50 = 8.9 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
107995 103901 20 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
29982233 103901 20 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
CHEMBL267723 103901 20 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
10809333 33964 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 33964 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 209533 19 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL1256645 209533 19 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL1814790 209533 19 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL62 209533 19 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
10712649 125985 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 125985 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1256645 209533 19 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1814790 209533 19 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL62 209533 19 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
10835172 125957 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 406 2 0 2 5.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL343078 125957 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 406 2 0 2 5.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1(C)C 10.1021/jm00022a004
10247592 35677 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 35677 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10525999 34136 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Br)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136776 34136 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Br)cc32)CC1(C)C 10.1021/jm00022a004
10574585 34198 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 34198 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
5016 115946 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL32145 115946 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL544114 115946 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
146025812 181670 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 181670 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10049758 211424 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL73589 211424 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
177725 180045 2 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)C[C@H]1c3c(ccc(O)c3O2)CCN1C 10.1021/jm060959i
CHEMBL452510 180045 2 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)C[C@H]1c3c(ccc(O)c3O2)CCN1C 10.1021/jm060959i
159034 180046 3 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1ccc2c(c1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL452512 180046 3 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1ccc2c(c1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
15657216 19769 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1189682 19769 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL539274 19769 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
15657214 20010 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1191339 20010 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL542419 20010 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
10252000 105323 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27650 105323 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50188 105323 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
15065270 119133 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 249 2 1 4 2.5 CCCN1CCC2=C(CCc3sc(N)nc32)C1 10.1021/jm00113a010
CHEMBL329444 119133 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 249 2 1 4 2.5 CCCN1CCC2=C(CCc3sc(N)nc32)C1 10.1021/jm00113a010
194775 214098 27 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 223 3 1 4 2.2 CCCN1CCC=C(c2csc(N)n2)C1 10.1021/jm00113a010
CHEMBL93428 214098 27 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 223 3 1 4 2.2 CCCN1CCC=C(c2csc(N)n2)C1 10.1021/jm00113a010
10008463 18021 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178971 18021 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51985 18021 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11743327 105478 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27763 105478 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
131001 105769 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27995 105769 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
10364722 105861 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 105861 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 105861 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 106335 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 106335 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9975915 106512 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL284912 106512 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10338595 169278 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL416747 169278 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10707563 35128 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
CHEMBL137478 35128 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
3082597 106335 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL283606 106335 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
14138285 151933 6 None - 1 Human 6.0 pIC50 = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
CHEMBL3912178 151933 6 None - 1 Human 6.0 pIC50 = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
71109989 160554 0 None 6 2 Human 7.0 pIC50 = 7.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3982119 160554 0 None 6 2 Human 7.0 pIC50 = 7.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
9992356 16528 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL113477 16528 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
440585 19463 15 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL1187468 19463 15 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL503882 19463 15 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
135221 151997 5 None - 1 Human 6.0 pIC50 = 6.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3912606 151997 5 None - 1 Human 6.0 pIC50 = 6.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
135398737 7745 93 None -44 90 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 7745 93 None -44 90 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 7745 93 None -44 90 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 7745 93 None -44 90 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 7745 93 None -44 90 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
10015045 20424 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
CHEMBL119455 20424 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
6603799 106490 17 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL284746 106490 17 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@H](c1ccccc1)CNCC2 10.1021/jm00086a016
150 9287 21 None -43 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 9287 21 None -43 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 9287 21 None -43 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 9287 21 None -43 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 9287 21 None -43 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
14901831 20156 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1192581 20156 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL543838 20156 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
3168 16034 92 None -89 22 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -89 22 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
16104 168696 19 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
CHEMBL415300 168696 19 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
16104 168696 19 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm9704457
CHEMBL415300 168696 19 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm9704457
6603820 102549 19 None 1 12 Rat 7.9 pIC50 = 7.9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 102549 19 None 1 12 Rat 7.9 pIC50 = 7.9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
1353 8692 93 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10015045 20424 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL119455 20424 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
146025812 181670 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 181670 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10043978 34021 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 34021 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
14901827 19825 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190039 19825 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL540036 19825 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
44584684 19214 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL1186001 19214 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL445011 19214 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
2398 7741 62 None -11 29 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 7741 62 None -11 29 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 7741 62 None -11 29 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 7741 62 None -11 29 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 7741 62 None -11 29 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
44317479 212524 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.
ChEMBL 243 4 3 3 2.4 NCC(Cc1ccccc1)c1ccc(O)c(O)c1 10.1021/jm00013a015
CHEMBL82706 212524 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.
ChEMBL 243 4 3 3 2.4 NCC(Cc1ccccc1)c1ccc(O)c(O)c1 10.1021/jm00013a015
10885636 117793 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 117793 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
10024827 19909 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1190552 19909 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL541096 19909 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
70684206 82840 0 None 11 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057442 82840 0 None 11 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692652 82839 0 None 8 2 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
CHEMBL2057441 82839 0 None 8 2 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
10547041 30586 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.8 Oc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
CHEMBL133615 30586 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.8 Oc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
14901829 19915 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190633 19915 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL541304 19915 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
10264849 16139 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 265 0 1 2 3.3 CN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
CHEMBL111348 16139 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 265 0 1 2 3.3 CN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
107715 207724 22 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
8447 195728 84 None -8 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 195728 84 None -8 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3191 109635 97 None -12 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -12 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
13154762 109887 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 109887 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
15648961 114178 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 341 2 0 1 5.4 CN1CCC(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL317982 114178 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 341 2 0 1 5.4 CN1CCC(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
6603820 102549 19 None 1 12 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00168a034
CHEMBL25856 102549 19 None 1 12 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00168a034
6917970 10463 61 None -1 33 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 10463 61 None -1 33 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 10463 61 None -1 33 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
6604005 163896 2 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm00168a034
CHEMBL407489 163896 2 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm00168a034
10361722 28992 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.5 Oc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
CHEMBL132304 28992 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.5 Oc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
10333742 66174 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 277 2 0 1 4.1 c1ccc(CN2CCCC3Cc4ccccc4CC32)cc1 10.1016/s0960-894x(01)00076-2
CHEMBL170974 66174 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 277 2 0 1 4.1 c1ccc(CN2CCCC3Cc4ccccc4CC32)cc1 10.1016/s0960-894x(01)00076-2
42 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
56971 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL8412 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
42 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
56971 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
CHEMBL8412 8844 57 None - 18 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
44370646 54989 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL155246 54989 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/jm00164a022
44269133 40709 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 356 2 3 3 2.1 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14239 40709 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 356 2 3 3 2.1 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
72329 102423 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 337 2 2 5 4.0 COc1c(O)c2c3c(nccc3c1OC)C(C)(C)c1cc(O)ccc1-2 10.1021/jm060959i
CHEMBL257958 102423 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 337 2 2 5 4.0 COc1c(O)c2c3c(nccc3c1OC)C(C)(C)c1cc(O)ccc1-2 10.1021/jm060959i
64143 205643 62 None -1 8 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 205643 62 None -1 8 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
10523361 36598 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC(C)N1C 10.1021/jm00022a004
CHEMBL138745 36598 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC(C)N1C 10.1021/jm00022a004
10567738 126184 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 320 2 0 2 4.3 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL344680 126184 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 320 2 0 2 4.3 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
71109797 152674 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 152674 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
135398737 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
38 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
722 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
CHEMBL42 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
DB00363 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
15653096 214669 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
CHEMBL1788129 214669 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
CHEMBL96618 214669 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
135398737 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
135398737 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
38 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
722 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
CHEMBL42 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
DB00363 7745 93 None -83 90 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
100 10577 58 None -16 54 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
2637 10577 58 None -16 54 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
5452 10577 58 None -16 54 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
CHEMBL479 10577 58 None -16 54 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
DB00679 10577 58 None -16 54 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
131213 12074 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL106622 12074 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
131213 12074 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL106622 12074 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
44312870 211356 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
CHEMBL73082 211356 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
44285576 149029 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C/c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
CHEMBL38848 149029 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C/c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
12545 54433 12 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 281 1 1 3 3.2 COc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL154709 54433 12 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 281 1 1 3 3.2 COc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
195158 49925 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
CHEMBL150550 49925 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
44267161 169821 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL417608 169821 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
70690498 82842 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 82842 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
71109805 94280 0 None 27 3 Human 7.8 pIC50 = 7.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
CHEMBL2334881 94280 0 None 27 3 Human 7.8 pIC50 = 7.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
70690500 82848 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 82848 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
70692653 82841 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057443 82841 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
70692653 82841 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 82841 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
146025817 182796 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
22857296 35923 0 None - 4 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13816 35923 0 None - 4 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
146025817 182796 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 182796 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
15720219 75440 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranesCompound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranes
ChEMBL 220 5 0 2 2.9 CCCN(CCC)[C@H]1CCn2cccc2C1 10.1016/S0960-894X(00)80003-7
CHEMBL192037 75440 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranesCompound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranes
ChEMBL 220 5 0 2 2.9 CCCN(CCC)[C@H]1CCn2cccc2C1 10.1016/S0960-894X(00)80003-7
146025813 182366 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6603820 102549 19 None 1 12 Rat 6.8 pIC50 = 6.8 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 102549 19 None 1 12 Rat 6.8 pIC50 = 6.8 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
2585 7590 103 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
71474024 151246 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3906676 151246 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
10247592 35677 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 35677 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
146025816 176757 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025816 176757 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 176757 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
44190762 183659 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 183659 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
26987 7736 33 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 7736 33 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 7736 33 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 7736 33 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 7736 33 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
9851833 19212 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL1185978 19212 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL443953 19212 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
2274 9947 58 None -16 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -16 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -16 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -16 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -16 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44284723 144899 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C/C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL37661 144899 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C/C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
277 8083 62 None -33 50 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 8083 62 None -33 50 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 8083 62 None -33 50 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 8083 62 None -33 50 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 8083 62 None -33 50 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
146025815 176558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
15115476 33879 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 2 0 2 4.2 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
CHEMBL136553 33879 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 2 0 2 4.2 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
10320519 33888 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 4 1 3 3.2 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL136562 33888 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 4 1 3 3.2 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
146025815 176558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 176558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
10732779 195050 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 297 4 2 3 3.7 CCCN1CCc2cc(O)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm001128u
CHEMBL49995 195050 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 297 4 2 3 3.7 CCCN1CCc2cc(O)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm001128u
10264176 118103 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL326781 118103 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
10048240 20166 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1192639 20166 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL543914 20166 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44358170 35060 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 378 2 0 2 4.7 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
CHEMBL137430 35060 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 378 2 0 2 4.7 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
100 10577 58 None -16 54 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
2637 10577 58 None -16 54 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
5452 10577 58 None -16 54 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
CHEMBL479 10577 58 None -16 54 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
DB00679 10577 58 None -16 54 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
44370644 55575 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm060959i
CHEMBL155884 55575 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm060959i
240 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
2769 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44279790 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
660 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL1729 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL560739 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
DB00604 7731 43 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44370644 55575 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
CHEMBL155884 55575 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
6603798 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL1613539 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL288096 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
6603798 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL1613539 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL288096 106956 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
14140118 102371 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 1 4 3.2 COc1c(O)c2c3c(c1OC)CCN(C)C3Cc1ccccc1-2 10.1021/jm060959i
CHEMBL257747 102371 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 1 4 3.2 COc1c(O)c2c3c(c1OC)CCN(C)C3Cc1ccccc1-2 10.1021/jm060959i
1043 8363 14 None -9549 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -9549 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -9549 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -9549 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -9549 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1588 9105 27 None -131 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None -131 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None -131 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None -131 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None -131 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
15653097 213971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL2111567 213971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL92560 213971 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
9979207 20610 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1195842 20610 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL555427 20610 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44370749 55513 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL155833 55513 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
70692652 82839 0 None 8 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057441 82839 0 None 8 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
6603729 106732 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL286424 106732 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@H](c2ccccc2)C1 10.1021/jm00086a016
192611 20341 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1193985 20341 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL545477 20341 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
10595484 125868 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)C(C)CN1C 10.1021/jm00022a004
CHEMBL342698 125868 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)C(C)CN1C 10.1021/jm00022a004
71240 214496 14 None - 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00072a006
CHEMBL95636 214496 14 None - 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00072a006
1241 106955 24 None -1 8 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL288090 106955 24 None -1 8 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL552611 106955 24 None -1 8 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
1242 10385 27 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
935 10385 27 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
CHEMBL286080 10385 27 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
44269117 104088 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 352 2 2 4 3.2 CN1C[C@H](C(=O)Nc2nccs2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL269160 104088 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 352 2 2 4 3.2 CN1C[C@H](C(=O)Nc2nccs2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
10831881 123250 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 4.1 I/C=C/CN1CCC[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm980284m
CHEMBL336128 123250 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 4.1 I/C=C/CN1CCC[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm980284m
71474025 152105 0 None 131 2 Human 5.7 pIC50 = 5.7 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 152105 0 None 131 2 Human 5.7 pIC50 = 5.7 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
135398737 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
38 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
722 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
CHEMBL42 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
DB00363 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
135398737 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
38 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
722 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
CHEMBL42 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
DB00363 7745 93 None -83 90 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
100 10577 58 None -47 54 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -47 54 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -47 54 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -47 54 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -47 54 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
129503 168447 10 None - 4 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL413105 168447 10 None - 4 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
2750 210840 76 None -5 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -5 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
10043978 34021 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 34021 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10641744 38102 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 352 2 0 2 4.7 Cc1ccc2c(c1)C(N1CCN(C)C(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL140189 38102 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 352 2 0 2 4.7 Cc1ccc2c(c1)C(N1CCN(C)C(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10810109 122273 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 Fc1ccc(C2CC(N3CCN4CCCCC4C3)c3cc(Cl)ccc32)cc1 10.1021/jm00022a004
CHEMBL335155 122273 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 Fc1ccc(C2CC(N3CCN4CCCCC4C3)c3cc(Cl)ccc32)cc1 10.1021/jm00022a004
9819535 105723 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.
ChEMBL 344 2 1 4 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(N=C=S)c2)C1 10.1016/0960-894X(96)00186-2
CHEMBL279634 105723 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.
ChEMBL 344 2 1 4 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(N=C=S)c2)C1 10.1016/0960-894X(96)00186-2
2726 7706 68 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
621 7706 68 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
83 7706 68 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
CHEMBL71 7706 68 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
DB00477 7706 68 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
12765746 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
12765746 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
1238 209953 24 None -5 16 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL64249 209953 24 None -5 16 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
12765746 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00072a006
10666149 126110 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 0 2 4.7 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
CHEMBL344216 126110 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 0 2 4.7 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
10246528 34065 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 34065 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
3036864 209533 19 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 209533 19 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 209533 19 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 209533 19 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
5018 10322 13 None 2 10 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 10322 13 None 2 10 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 10322 13 None 2 10 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 10322 13 None 2 10 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
10810514 33989 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 392 2 1 2 5.1 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CCN1 10.1021/jm00022a004
CHEMBL136648 33989 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 392 2 1 2 5.1 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CCN1 10.1021/jm00022a004
135514603 210893 14 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL70319 210893 14 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
681 8247 72 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
940 8247 72 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
947 8247 72 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
CHEMBL59 8247 72 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
DB00988 8247 72 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
15653098 214027 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1 10.1021/jm00022a004
CHEMBL92896 214027 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1 10.1021/jm00022a004
121852 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9978353 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL1178987 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL52785 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
9981024 102872 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 102872 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 102872 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10319624 105763 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27991 105763 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL298534 105763 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9980269 105859 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280586 105859 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54266 105859 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10321248 106202 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28287 106202 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50722 106202 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 16938 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
10333685 95319 3 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 276 1 1 1 3.8 CN1CCc2c([nH]c3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
CHEMBL23529 95319 3 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 276 1 1 1 3.8 CN1CCc2c([nH]c3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
14233815 213785 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CCC21 10.1021/jm00113a010
CHEMBL91453 213785 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CCC21 10.1021/jm00113a010
71109993 150025 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
CHEMBL3896617 150025 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
14547414 109061 1 None - 4 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL303339 109061 1 None - 4 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
28417 46813 49 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
10480509 149109 0 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388564 149109 0 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
44312605 211214 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL72162 211214 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
44323851 213753 0 None 3 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL91310 213753 0 None 3 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
13154801 34224 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 370 5 1 4 3.0 COc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136841 34224 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 370 5 1 4 3.0 COc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
24121307 109820 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(C)(=O)=O)cc32)CC1 10.1021/jm991005d
CHEMBL307163 109820 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(C)(=O)=O)cc32)CC1 10.1021/jm991005d
3117 214620 103 None -2 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
147080 212755 5 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.
ChEMBL 365 6 0 6 2.8 O=c1ccoc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1021/jm00105a039
CHEMBL84639 212755 5 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.
ChEMBL 365 6 0 6 2.8 O=c1ccoc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1021/jm00105a039
44354812 31901 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 3.8 I/C=C/CN1CCCC2Cc3ccccc3CC21 10.1021/jm980284m
CHEMBL134746 31901 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 3.8 I/C=C/CN1CCCC2Cc3ccccc3CC21 10.1021/jm980284m
44285034 156546 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C\C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL39483 156546 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C\C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
135493554 210939 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3cc(OS(C)(=O)=O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL70609 210939 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3cc(OS(C)(=O)=O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
125720 33087 5 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 338 2 2 3 1.7 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13588 33087 5 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 338 2 2 3 1.7 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
9911120 16395 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 16395 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
2726 7706 68 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
4913274 24772 2 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 408 4 1 3 4.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
CHEMBL12628 24772 2 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 408 4 1 3 4.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
15648962 115129 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 339 2 0 1 5.3 CN1CC=C(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL319810 115129 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 339 2 0 1 5.3 CN1CC=C(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
1212 8443 50 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
146025814 179558 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
9911120 16395 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 16395 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
11744707 171688 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL422283 171688 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
228 7233 28 None -30 23 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
33 7233 28 None -30 23 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
6005 7233 28 None -30 23 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
CHEMBL53 7233 28 None -30 23 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
DB00714 7233 28 None -30 23 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
10400783 201664 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 267 2 1 3 2.8 c1ccc(C[C@@H]2NCCc3cc4c(cc32)OCO4)cc1 10.1021/jm001128u
CHEMBL54051 201664 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 267 2 1 3 2.8 c1ccc(C[C@@H]2NCCc3cc4c(cc32)OCO4)cc1 10.1021/jm001128u
10531 8202 21 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
440989 102075 27 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 285 3 3 4 2.5 COc1cc2c(cc1O)[C@@H](Cc1ccc(O)cc1)NCC2 10.1021/np980008a
CHEMBL256448 102075 27 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 285 3 3 4 2.5 COc1cc2c(cc1O)[C@@H](Cc1ccc(O)cc1)NCC2 10.1021/np980008a
10408602 20468 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1194852 20468 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL553399 20468 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
2284 9956 33 None -36 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 9956 33 None -36 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 9956 33 None -36 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 9956 33 None -36 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 9956 33 None -36 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
10246528 34065 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 34065 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
22179 193044 42 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 3 5 2.5 COc1cc2c(cc1O)C[C@@H]1NCCc3cc(O)c(OC)c-2c31 10.1021/jm060959i
CHEMBL487388 193044 42 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 3 5 2.5 COc1cc2c(cc1O)C[C@@H]1NCCc3cc(O)c(OC)c-2c31 10.1021/jm060959i
11035765 16660 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
CHEMBL114280 16660 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
49836496 25327 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
CHEMBL1275791 25327 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
146025814 179558 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 179558 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
197505 20463 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1194829 20463 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL553361 20463 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
441383 27105 57 None -12 17 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -12 17 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
2600 10551 74 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 10551 74 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 10551 74 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 10551 74 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 10551 74 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
10762505 171636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 4.1 COc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
CHEMBL421914 171636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 4.1 COc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
2477 7532 59 None -28 29 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
36 7532 59 None -28 29 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
437 7532 59 None -28 29 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL49 7532 59 None -28 29 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
DB00490 7532 59 None -28 29 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
44342270 16702 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 16702 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
2286 9957 51 None -30 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 9957 51 None -30 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 9957 51 None -30 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 9957 51 None -30 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 9957 51 None -30 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
11730467 17800 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 17800 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11080 35858 79 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 35858 79 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
5352624 74013 44 None -3 5 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
CHEMBL18797 74013 44 None -3 5 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
2662 18156 131 None -3 30 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 18156 131 None -3 30 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
13154762 109887 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 109887 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
6603997 106686 12 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL286120 106686 12 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00086a016
15723883 212898 1 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 294 6 0 2 3.8 c1ccc(CCCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm00116a003
CHEMBL85879 212898 1 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 294 6 0 2 3.8 c1ccc(CCCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm00116a003
31101 7516 40 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 7516 40 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 7516 40 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 7516 40 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 7516 40 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10264175 115378 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@@H]21 10.1021/jm00002a013
CHEMBL320481 115378 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@@H]21 10.1021/jm00002a013
196129 74573 17 None -1819 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 74573 17 None -1819 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
70684207 82845 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057452 82845 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70684207 82845 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057452 82845 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
14547415 107447 1 None - 4 Rat 4.5 pIC50 = 4.5 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL292274 107447 1 None - 4 Rat 4.5 pIC50 = 4.5 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
73453 36389 24 None -208 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 36389 24 None -208 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
195158 49925 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
CHEMBL150550 49925 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
21589014 150850 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3903297 150850 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
10246528 34065 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 34065 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
10004036 102004 0 None 33 2 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL256075 102004 0 None 33 2 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
10570260 35214 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(F)c32)CC1(C)C 10.1021/jm00022a004
CHEMBL137536 35214 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(F)c32)CC1(C)C 10.1021/jm00022a004
70692655 82849 0 None 8 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057456 82849 0 None 8 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
15723897 16266 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 330 5 0 2 4.6 c1ccc(N2CCN(CCCc3ccc4ccccc4c3)CC2)cc1 10.1021/jm00116a003
CHEMBL112037 16266 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 330 5 0 2 4.6 c1ccc(N2CCN(CCCc3ccc4ccccc4c3)CC2)cc1 10.1021/jm00116a003
228 7233 28 None -30 23 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
33 7233 28 None -30 23 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
6005 7233 28 None -30 23 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
CHEMBL53 7233 28 None -30 23 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
DB00714 7233 28 None -30 23 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
681 8247 72 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
940 8247 72 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
947 8247 72 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
CHEMBL59 8247 72 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
DB00988 8247 72 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
9861399 40071 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 307 2 0 2 4.9 CCN1CCc2c(sc3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
CHEMBL141863 40071 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 307 2 0 2 4.9 CCN1CCc2c(sc3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
10251234 18017 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 18017 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 18017 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10429859 18814 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL1183429 18814 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL296395 18814 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
10476735 20503 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1195096 20503 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL553833 20503 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 102872 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 102872 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 102872 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
44312603 110550 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 350 1 0 2 4.9 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL308843 110550 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 350 1 0 2 4.9 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
14728694 12121 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 2 0 3 4.1 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/jm00174a002
CHEMBL106886 12121 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 2 0 3 4.1 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/jm00174a002
44319215 19976 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1191117 19976 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL542167 19976 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
11057 182928 23 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 182928 23 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 182928 23 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 182928 23 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
10809334 33620 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1(C)C 10.1021/jm00022a004
CHEMBL136334 33620 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1(C)C 10.1021/jm00022a004
6761 74574 19 None -5 18 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 74574 19 None -5 18 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44285043 161589 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C\c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
CHEMBL40031 161589 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C\c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
10043093 210638 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(Br)cc3CC[C@H]21 10.1021/jm00002a013
CHEMBL68680 210638 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(Br)cc3CC[C@H]21 10.1021/jm00002a013
70690497 82838 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057438 82838 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
70690497 82838 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL2057438 82838 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
13994412 17936 1 None -117 3 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL117841 17936 1 None -117 3 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
7055406 196122 3 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 299 4 2 4 2.8 COc1ccc(C[C@H]2NCCc3cc(O)c(OC)cc32)cc1 10.1021/np980008a
CHEMBL512542 196122 3 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 299 4 2 4 2.8 COc1ccc(C[C@H]2NCCc3cc(O)c(OC)cc32)cc1 10.1021/np980008a
9816455 23563 8 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@H]2CNC3 10.1021/jm0101545
CHEMBL124561 23563 8 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@H]2CNC3 10.1021/jm0101545
130907 201462 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL53294 201462 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
10091430 16653 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
CHEMBL11425 16653 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
457825 179433 40 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
CHEMBL449690 179433 40 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
CHEMBL506025 179433 40 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
130907 201462 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL53294 201462 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
44370718 126318 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
CHEMBL345822 126318 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
1353 8692 93 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
3559 8692 93 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
86 8692 93 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
CHEMBL54 8692 93 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
DB00502 8692 93 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
10548369 37218 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 388 2 0 2 5.6 CN1CCN(C2CC(c3ccc(Cl)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL139258 37218 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 388 2 0 2 5.6 CN1CCN(C2CC(c3ccc(Cl)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
9979258 104892 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 415 3 2 2 4.9 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL273526 104892 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 415 3 2 2 4.9 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
44267181 16383 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11262 16383 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
6852376 98374 13 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL1467585 98374 13 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL24077 98374 13 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL503958 98374 13 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
44269085 31761 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13464 31761 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
180 7189 56 None -109 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 7189 56 None -109 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 7189 56 None -109 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 7189 56 None -109 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 7189 56 None -109 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
1353 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
3559 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
86 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
CHEMBL54 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
DB00502 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
1353 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
3559 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
86 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
CHEMBL54 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
DB00502 8692 93 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
164710 102370 7 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 4 2.5 Oc1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
CHEMBL257746 102370 7 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 4 2.5 Oc1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
736083 168993 17 None -50 2 Rat 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00164a022
CHEMBL416288 168993 17 None -50 2 Rat 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00164a022
10619325 34282 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136891 34282 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1(C)C 10.1021/jm00022a004
71110290 153938 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3927835 153938 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
681 8247 72 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
940 8247 72 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
947 8247 72 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
CHEMBL59 8247 72 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
DB00988 8247 72 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
4011 89183 49 None -64 24 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 89183 49 None -64 24 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
11005810 17238 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 17238 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44358128 33786 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 324 2 0 2 4.0 Cc1ccc2c(c1)C(N1CCN(C)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136480 33786 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 324 2 0 2 4.0 Cc1ccc2c(c1)C(N1CCN(C)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
14901835 19687 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
CHEMBL1189074 19687 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
CHEMBL538012 19687 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
10527884 35147 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
CHEMBL137486 35147 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
44269075 35392 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13770 35392 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
10550367 121985 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
CHEMBL334498 121985 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
2351 10059 64 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
12488 8438 56 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 8438 56 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 8438 56 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 8438 56 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
13154803 123527 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 386 5 1 4 3.7 CSc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL337542 123527 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 386 5 1 4 3.7 CSc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
100231 184697 7 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL451211 184697 7 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL464525 184697 7 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
191 7191 98 None -26 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 7191 98 None -26 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 7191 98 None -26 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 7191 98 None -26 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 7191 98 None -26 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
121852 16938 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11592 16938 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL301060 16938 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
10452020 125053 3 None - 3 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL34095 125053 3 None - 3 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm00086a016
3036864 209533 19 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL1256645 209533 19 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL1814790 209533 19 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL62 209533 19 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
3036864 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
3036864 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 209533 19 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
10809335 33772 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccccc3F)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136468 33772 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccccc3F)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
70690500 82848 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 82848 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
3496768 102515 4 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 0 1 4 2.9 CN1CCc2cc3c(c4c2C1Cc1cccc(O)c1-4)OCO3 10.1021/jm060959i
CHEMBL258370 102515 4 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 0 1 4 2.9 CN1CCc2cc3c(c4c2C1Cc1cccc(O)c1-4)OCO3 10.1021/jm060959i
10154 148907 59 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL388342 148907 59 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
10154 148907 59 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388342 148907 59 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
9981671 21313 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL12028 21313 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
121852 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251234 18017 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 18017 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 18017 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10047322 103915 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL26783 103915 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL50993 103915 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
10251673 106266 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283207 106266 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52396 106266 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10070029 172196 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL423841 172196 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54089 172196 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10265863 200103 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
CHEMBL52438 200103 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
121852 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 16938 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
2247 7293 81 None -61 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -61 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -61 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -61 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -61 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
134551 7146 27 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
146025811 178540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 178540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025811 178540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 178540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
5353853 24758 47 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10498684 38413 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 359 3 2 2 3.6 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL14048 38413 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 359 3 2 2 3.6 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
71474079 150042 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3896731 150042 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
2337 10030 77 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 10030 77 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 10030 77 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 10030 77 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 10030 77 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
11016 210386 38 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 173 3 0 1 0.0 O=P(N1CC1)(N1CC1)N1CC1 10.1021/jm980284m
CHEMBL670 210386 38 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 173 3 0 1 0.0 O=P(N1CC1)(N1CC1)N1CC1 10.1021/jm980284m
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
332915 36491 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 240 0 1 1 3.1 C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL13866 36491 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 240 0 1 1 3.1 C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
10712649 125985 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 125985 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
5353432 104271 89 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 104271 89 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
44323870 118368 0 None 3 4 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL328246 118368 0 None 3 4 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
228 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
33 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
6005 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
CHEMBL53 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
DB00714 7233 28 None -30 23 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
9864292 36881 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL138964 36881 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1(C)C 10.1021/jm00022a004
70682088 82843 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 82843 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
14004813 66058 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 307 3 0 2 4.1 COc1cccc2c1CC1CCCN(Cc3ccccc3)C1C2 10.1016/s0960-894x(01)00076-2
CHEMBL170475 66058 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 307 3 0 2 4.1 COc1cccc2c1CC1CCCN(Cc3ccccc3)C1C2 10.1016/s0960-894x(01)00076-2
CHEMBL1200633 215379 3 None -7 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
44269057 38117 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 412 2 3 3 3.4 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14020 38117 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 412 2 3 3 3.4 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
71110293 150157 0 None 6 3 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 150157 0 None 6 3 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
2389 10104 118 None -489 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 10104 118 None -489 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 10104 118 None -489 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 10104 118 None -489 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 10104 118 None -489 66 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
44358098 126062 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 292 2 0 2 3.5 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
CHEMBL343820 126062 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 292 2 0 2 3.5 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
133381 102369 9 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 4 2.8 COc1c2c3c(c4c1OCO4)-c1ccccc1C[C@H]3NCC2 10.1021/jm060959i
CHEMBL257745 102369 9 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 4 2.8 COc1c2c3c(c4c1OCO4)-c1ccccc1C[C@H]3NCC2 10.1021/jm060959i
71110293 150157 0 None 6 3 Human 6.3 pIC50 = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 150157 0 None 6 3 Human 6.3 pIC50 = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
71474026 161078 0 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
CHEMBL3986624 161078 0 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
45482789 205704 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 205704 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
5024 126028 25 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 297 3 0 3 3.3 COc1cc2c(cc1OC)C(c1ccccc1)CN(C)CC2 10.1021/jm980156y
CHEMBL343569 126028 25 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 297 3 0 3 3.3 COc1cc2c(cc1OC)C(c1ccccc1)CN(C)CC2 10.1021/jm980156y
10742 10389 31 None 2 8 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
1225 10389 31 None 2 8 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
CHEMBL35354 10389 31 None 2 8 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
13154762 109887 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 109887 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
6603820 102549 19 None 1 12 Rat 8.3 pIC50 = 8.3 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 102549 19 None 1 12 Rat 8.3 pIC50 = 8.3 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
10617001 37929 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 1 2 4.4 Cc1ccc2c(c1)C(N1CCNC(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL140032 37929 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 1 2 4.4 Cc1ccc2c(c1)C(N1CCNC(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
6852376 98374 13 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL1467585 98374 13 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL24077 98374 13 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL503958 98374 13 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
11794523 37011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 385 2 0 2 5.7 CCN1CCc2c(sc3ccccc23)C(c2cccc(Br)c2)C1 10.1021/jm980156y
CHEMBL139081 37011 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 385 2 0 2 5.7 CCN1CCc2c(sc3ccccc23)C(c2cccc(Br)c2)C1 10.1021/jm980156y
10712993 125526 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 352 3 0 4 4.8 CCN1CCc2c(sc3ccccc23)C(c2cccc([N+](=O)[O-])c2)C1 10.1021/jm980156y
CHEMBL341805 125526 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 352 3 0 4 4.8 CCN1CCc2c(sc3ccccc23)C(c2cccc([N+](=O)[O-])c2)C1 10.1021/jm980156y
10251234 18017 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 18017 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 18017 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364722 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10072866 204254 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51561 204254 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL56990 204254 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11099480 195924 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1ccc2c(c1O)Oc1c(OC)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL510777 195924 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1ccc2c(c1O)Oc1c(OC)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
44370629 57833 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
CHEMBL157879 57833 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
10246432 20573 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1195595 20573 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL554950 20573 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44379650 127535 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL355107 127535 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
10574585 34198 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 34198 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
13154795 35673 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 4 1 3 3.3 Cc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL137954 35673 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 4 1 3 3.3 Cc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10582557 201509 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 309 4 0 3 4.0 CCCN1CCc2cc3c(cc2[C@@H]1Cc1ccccc1)OCO3 10.1021/jm001128u
CHEMBL53520 201509 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 309 4 0 3 4.0 CCCN1CCc2cc3c(cc2[C@@H]1Cc1ccccc1)OCO3 10.1021/jm001128u
11795296 33540 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 33540 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10424479 115645 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 293 2 1 2 4.1 CCCN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
CHEMBL321040 115645 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 293 2 1 2 4.1 CCCN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
10923047 23281 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@@H]2CNC3 10.1021/jm0101545
CHEMBL123642 23281 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@@H]2CNC3 10.1021/jm0101545
1971 9641 38 None -8 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 9641 38 None -8 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 9641 38 None -8 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 9641 38 None -8 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 9641 38 None -8 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
44312870 211356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL73082 211356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
44323876 213361 0 None 2 4 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL88870 213361 0 None 2 4 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
135 9310 43 None -91 56 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 9310 43 None -91 56 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 9310 43 None -91 56 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 9310 43 None -91 56 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 9310 43 None -91 56 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
10828627 109941 20 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm991005d
CHEMBL308090 109941 20 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm991005d
15521599 211317 9 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm991005d
CHEMBL72794 211317 9 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm991005d
10828627 109941 20 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm9704457
CHEMBL308090 109941 20 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm9704457
15521599 211317 9 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm9704457
CHEMBL72794 211317 9 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm9704457
10264174 16460 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@H]21 10.1021/jm00002a013
CHEMBL113053 16460 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@H]21 10.1021/jm00002a013
70692656 82850 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057457 82850 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692656 82850 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 82850 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
10031670 19236 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL1186148 19236 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL451734 19236 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
44370651 53524 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1c(Cl)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL153960 53524 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1c(Cl)ccc(O)c1-3 10.1021/jm00164a022
3561 25849 39 None -1 11 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 25849 39 None -1 11 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
14137099 179470 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
CHEMBL450147 179470 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
CHEMBL507970 179470 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
44269131 37684 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 381 2 2 4 3.2 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13979 37684 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 381 2 2 4 3.2 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
71041800 169520 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 290 7 3 6 2.2 CCC[C@@H](CCO)Nc1nc(N)nc2cc(OC)ccc12 10.1021/acs.jmedchem.8b00643
CHEMBL4171368 169520 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 290 7 3 6 2.2 CCC[C@@H](CCO)Nc1nc(N)nc2cc(OC)ccc12 10.1021/acs.jmedchem.8b00643
44285013 160519 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 319 7 0 1 5.4 C(=C\C1CCCN(CCCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL39818 160519 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 319 7 0 1 5.4 C(=C\C1CCCN(CCCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
1042 8362 23 None -204 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 8362 23 None -204 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 8362 23 None -204 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 8362 23 None -204 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 8362 23 None -204 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
10693049 126146 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 412 2 0 2 6.0 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCCC2 10.1021/jm00022a004
CHEMBL344426 126146 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 412 2 0 2 6.0 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCCC2 10.1021/jm00022a004
10810927 126074 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 126074 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
146299 180156 8 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL452776 180156 8 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
44267790 22295 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 431 6 1 10 1.9 Cc1sc2nc(SCCCN3CCN(c4ncccn4)CC3)n(N)c(=O)c2c1C 10.1021/jm950866t
CHEMBL12177 22295 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 431 6 1 10 1.9 Cc1sc2nc(SCCCN3CCN(c4ncccn4)CC3)n(N)c(=O)c2c1C 10.1021/jm950866t
118731187 124957 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 613 10 3 7 6.1 CCOc1nc(NC(=O)C(C)(C)NC(=O)c2ccc3c(C4CCCC4)c(-c4ccc(F)cn4)n(C)c3c2)ccc1/C=C/C(=O)O 10.1016/j.bmcl.2014.12.078
CHEMBL3408841 124957 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 613 10 3 7 6.1 CCOc1nc(NC(=O)C(C)(C)NC(=O)c2ccc3c(C4CCCC4)c(-c4ccc(F)cn4)n(C)c3c2)ccc1/C=C/C(=O)O 10.1016/j.bmcl.2014.12.078
10092409 18818 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1183479 18818 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL299561 18818 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10095594 19140 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1185501 19140 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL417550 19140 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364722 105861 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 105861 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 105861 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL3215298 218010 13 None -6 2 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(C=C[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(C=C[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
14901811 20309 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1193777 20309 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL545240 20309 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
10809333 33964 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 33964 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
4189 213701 96 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
16104 168696 19 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00130a006
CHEMBL415300 168696 19 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00130a006
16104 168696 19 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00164a053
CHEMBL415300 168696 19 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00164a053
44285030 139268 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 291 5 0 1 4.7 C(=C\C1CCCN(CCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL36979 139268 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 291 5 0 1 4.7 C(=C\C1CCCN(CCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
23930365 102422 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c3c(c1OC)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1021/jm060959i
CHEMBL257957 102422 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c3c(c1OC)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1021/jm060959i
44370725 126330 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(Cl)c(O)c1-3 10.1021/jm00164a022
CHEMBL345907 126330 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(Cl)c(O)c1-3 10.1021/jm00164a022
9954899 211242 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 211242 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
9954899 211242 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
CHEMBL72292 211242 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
167715 9651 14 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
969 9651 14 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
CHEMBL225230 9651 14 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
71109986 157412 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
CHEMBL3955446 157412 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
9904738 108433 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 309 2 2 3 3.8 CCCN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
CHEMBL299161 108433 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 309 2 2 3 3.8 CCCN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
13154798 33543 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 382 5 1 3 4.1 CC(C)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136262 33543 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 382 5 1 3 4.1 CC(C)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10026300 174613 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 174613 17 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
10409038 92017 0 None -41 4 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL225853 92017 0 None -41 4 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
3081681 105290 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
compound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissuecompound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
CHEMBL276175 105290 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
compound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissuecompound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
5249490 21930 1 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1C2CNC3 10.1021/jm0101545
CHEMBL120995 21930 1 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1C2CNC3 10.1021/jm0101545
2105 9828 37 None -123 32 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 9828 37 None -123 32 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 9828 37 None -123 32 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 9828 37 None -123 32 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 9828 37 None -123 32 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
70690499 82846 0 None 9 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057453 82846 0 None 9 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
160597 161854 30 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 3 2.8 c1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
CHEMBL401798 161854 30 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 3 2.8 c1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
70682090 82844 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057451 82844 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70682090 82844 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057451 82844 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
3158 63041 27 None -2398 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 63041 27 None -2398 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
2601 10552 33 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
443951 10552 33 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
56 10552 33 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
CHEMBL73151 10552 33 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
DB13399 10552 33 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
13154822 37264 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 418 5 1 5 2.4 CS(=O)(=O)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL139304 37264 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 418 5 1 5 2.4 CS(=O)(=O)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
6603820 102549 19 None 1 12 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL25856 102549 19 None 1 12 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
71474025 152105 0 None 131 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 152105 0 None 131 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
11539632 77336 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 77336 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44354823 31346 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 241 1 1 2 2.2 C#CCN1CCCC2Cc3c(O)cccc3CC21 10.1021/jm980284m
CHEMBL134273 31346 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 241 1 1 2 2.2 C#CCN1CCCC2Cc3c(O)cccc3CC21 10.1021/jm980284m
16038374 101122 95 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
ChEMBL 357 5 1 4 4.9 COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1 10.1073/pnas.0611364104
CHEMBL250699 101122 95 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
ChEMBL 357 5 1 4 4.9 COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1 10.1073/pnas.0611364104
10571551 123345 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 375 2 0 2 6.2 CCN1CCc2c(sc3ccccc23)C(c2ccc(Cl)c(Cl)c2)C1 10.1021/jm980156y
CHEMBL336437 123345 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 375 2 0 2 6.2 CCN1CCc2c(sc3ccccc23)C(c2ccc(Cl)c(Cl)c2)C1 10.1021/jm980156y
135398745 9688 112 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
49836386 25322 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
CHEMBL1275709 25322 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
44269142 38903 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL14089 38903 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
15115475 33618 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 322 4 1 3 2.9 OCCN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
CHEMBL136333 33618 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 322 4 1 3 2.9 OCCN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
12441 57865 21 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm00164a022
CHEMBL157912 57865 21 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm00164a022
44269091 105197 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL275539 105197 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
44312604 211230 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 338 1 0 2 4.6 CC1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL72220 211230 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 338 1 0 2 4.6 CC1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
133 9274 52 None -30 43 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -30 43 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -30 43 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -30 43 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -30 43 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
12441 57865 21 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm060959i
CHEMBL157912 57865 21 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm060959i
5018 10322 13 None 2 10 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 10322 13 None 2 10 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 10322 13 None 2 10 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 10322 13 None 2 10 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
135686415 211355 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm991005d
CHEMBL73074 211355 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm991005d
135686415 211355 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm9704457
CHEMBL73074 211355 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm9704457
3294 8787 111 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
71360 8787 111 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
87 8787 111 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
CHEMBL14376 8787 111 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
DB04946 8787 111 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
10144 145188 46 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 275 0 0 4 3.2 O=C1c2ccccc2-c2c3c(cc4ccnc1c24)OCO3 10.1021/jm060959i
CHEMBL37736 145188 46 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 275 0 0 4 3.2 O=C1c2ccccc2-c2c3c(cc4ccnc1c24)OCO3 10.1021/jm060959i
44269092 35859 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 296 0 1 1 4.4 C[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL13811 35859 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 296 0 1 1 4.4 C[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
11059058 16863 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 16863 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
71110287 153103 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3921127 153103 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
448537 167029 89 None -28 25 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 167029 89 None -28 25 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44312605 211214 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
CHEMBL72162 211214 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
13720693 106449 4 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL284473 106449 4 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00086a016
71109897 94288 0 None 7 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
CHEMBL2334893 94288 0 None 7 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
10478809 171657 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
CHEMBL422067 171657 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
10787201 35505 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 4 0 2 5.9 CCC1(CC)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
CHEMBL137805 35505 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 4 0 2 5.9 CCC1(CC)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
44354809 123320 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 3.8 COc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
CHEMBL336274 123320 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 3.8 COc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
100 10577 58 None -16 54 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
2637 10577 58 None -16 54 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
5452 10577 58 None -16 54 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
CHEMBL479 10577 58 None -16 54 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
DB00679 10577 58 None -16 54 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
681 8247 72 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
940 8247 72 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
947 8247 72 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
CHEMBL59 8247 72 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
DB00988 8247 72 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
442203 181337 5 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1cc2c(cc1OC)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL455633 181337 5 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1cc2c(cc1OC)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
10504100 54514 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL154787 54514 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
14901825 19860 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190275 19860 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL540546 19860 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
10024943 104165 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26975 104165 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52485 104165 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10406315 200104 0 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL524439 200104 0 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
146025813 182366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 182366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44370706 54746 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1cc(Br)cc(O)c1-3 10.1021/jm00164a022
CHEMBL154989 54746 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1cc(Br)cc(O)c1-3 10.1021/jm00164a022
10409556 169151 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
CHEMBL416523 169151 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
15657207 213116 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 287 2 2 2 3.7 CNC1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL87321 213116 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 287 2 2 2 3.7 CNC1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00069a013
44269058 38140 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14022 38140 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
1016 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44370645 126340 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL346017 126340 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
1530 8963 50 None -53 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 8963 50 None -53 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 8963 50 None -53 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 8963 50 None -53 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 8963 50 None -53 21 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
10522247 33504 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 33504 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
16103 211417 47 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00130a006
CHEMBL73538 211417 47 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00130a006
16103 211417 47 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00164a053
CHEMBL73538 211417 47 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00164a053
71454427 85295 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL2111937 85295 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
44329358 114301 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL318714 114301 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
10833129 34263 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3cccc(F)c3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136873 34263 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3cccc(F)c3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
15648963 23666 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 340 2 0 2 5.1 CN1CC=C(c2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm00072a006
CHEMBL12507 23666 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 340 2 0 2 5.1 CN1CC=C(c2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm00072a006
70690500 82848 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 82848 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
9804849 74230 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 74230 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
2812 11551 101 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44584686 19464 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL1187479 19464 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL504303 19464 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
11543723 195878 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
CHEMBL51017 195878 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
176 7186 66 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
3198 212292 76 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
114876 19565 5 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
CHEMBL1188090 19565 5 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
CHEMBL545783 19565 5 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
135515198 111527 8 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL310712 111527 8 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
135515198 111527 8 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
CHEMBL310712 111527 8 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
134 9292 24 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 9292 24 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 9292 24 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 9292 24 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 9292 24 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
11778475 170074 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3ccc(O)c(O)c3CC[C@H]21 10.1021/jm00002a013
CHEMBL418791 170074 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3ccc(O)c(O)c3CC[C@H]21 10.1021/jm00002a013
66572162 82470 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 363 6 1 3 5.2 OC(CCN1CC=C(Cc2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.ejmech.2012.04.030
CHEMBL2047561 82470 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 363 6 1 3 5.2 OC(CCN1CC=C(Cc2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.ejmech.2012.04.030
10907460 16600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 16600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
25053021 116449 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL322574 116449 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
25053021 116449 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL322574 116449 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
70686343 82847 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057454 82847 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
135508767 210904 21 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL70377 210904 21 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
13891896 195710 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 297 2 2 4 2.8 COc1c(O)c2c3c(c1OC)CCN[C@@H]3Cc1ccccc1-2 10.1021/jm060959i
CHEMBL508011 195710 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 297 2 2 4 2.8 COc1c(O)c2c3c(c1OC)CCN[C@@H]3Cc1ccccc1-2 10.1021/jm060959i
135508767 210904 21 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
CHEMBL70377 210904 21 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
3082777 175101 10 None - 1 Human 9.8 pKd = 9.8 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2C(c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00119a003
CHEMBL434215 175101 10 None - 1 Human 9.8 pKd = 9.8 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2C(c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00119a003
164612037 192156 0 None -144 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -144 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 199747 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 199798 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 199810 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
44366049 50229 0 None - 1 Human 9.6 pKd = 9.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
CHEMBL150800 50229 0 None - 1 Human 9.6 pKd = 9.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
2869 10924 89 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60 10924 89 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60857 10924 89 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
CHEMBL1185 10924 89 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
DB00315 10924 89 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
3036864 209533 19 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL1256645 209533 19 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL1814790 209533 19 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL62 209533 19 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
129244 125449 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL2114388 125449 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL34170 125449 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
118736406 125734 0 None 3 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 673 16 7 7 2.7 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423404 125734 0 None 3 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 673 16 7 7 2.7 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
16731521 92230 0 None - 1 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 630 10 4 5 3.5 CC(C)[C@H](NC(=O)[C@H](CCC1CCCCC1)NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL226639 92230 0 None - 1 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 630 10 4 5 3.5 CC(C)[C@H](NC(=O)[C@H](CCC1CCCCC1)NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
118736409 125737 0 None -1 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 693 16 6 6 3.3 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423407 125737 0 None -1 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 693 16 6 6 3.3 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
6852376 98374 13 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL1467585 98374 13 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL24077 98374 13 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL503958 98374 13 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
118736412 125741 0 None -6 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423410 125741 0 None -6 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736405 125733 0 None -9 3 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423403 125733 0 None -9 3 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736413 125742 0 None -2 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423411 125742 0 None -2 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
167715 9651 14 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
969 9651 14 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
CHEMBL225230 9651 14 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
1153 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
12668023 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026874 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026875 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
3341 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
6603851 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
933 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
939 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
985 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1160786 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1161520 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL588 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
DB00800 8409 58 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
118736408 125736 0 None 1 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 696 16 7 6 3.5 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423406 125736 0 None 1 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 696 16 7 6 3.5 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
5311428 106883 9 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1744078 106883 9 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL287504 106883 9 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
10088113 169056 6 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1744079 169056 6 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL416401 169056 6 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
118736412 125741 0 None -6 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423410 125741 0 None -6 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
681 8247 72 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
940 8247 72 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
947 8247 72 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
CHEMBL59 8247 72 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
DB00988 8247 72 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
118736402 125730 0 None -5 4 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 659 11 5 6 2.4 CCCC[C@H](NC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423400 125730 0 None -5 4 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 659 11 5 6 2.4 CCCC[C@H](NC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
1153 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
12668023 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026874 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026875 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
3341 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
6603851 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
933 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
939 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
985 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1160786 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1161520 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL588 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
DB00800 8409 58 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
118736404 125732 0 None -2 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 18 7 7 3.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423402 125732 0 None -2 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 18 7 7 3.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736413 125742 0 None -2 2 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423411 125742 0 None -2 2 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736411 125739 0 None -1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 788 22 7 7 3.8 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423409 125739 0 None -1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 788 22 7 7 3.8 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
118736407 125735 0 None 1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 17 7 7 3.5 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423405 125735 0 None 1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 17 7 7 3.5 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
118736403 125731 0 None -6 3 Human 4.4 pKd = 4.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 786 22 8 8 3.4 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423401 125731 0 None -6 3 Human 4.4 pKd = 4.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 786 22 8 8 3.4 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
10452020 125053 3 None 10 3 Human 6.4 pKd = 6.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm950447w
CHEMBL34095 125053 3 None 10 3 Human 6.4 pKd = 6.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm950447w
118736410 125738 0 None -1 3 Human 5.4 pKd = 5.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 772 17 6 7 3.1 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423408 125738 0 None -1 3 Human 5.4 pKd = 5.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 772 17 6 7 3.1 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
122132 209343 17 None -87 4 Human 5.3 pKd = 5.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm950447w
CHEMBL611801 209343 17 None -87 4 Human 5.3 pKd = 5.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm950447w
1960 9632 67 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
439260 9632 67 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
505 9632 67 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
CHEMBL1437 9632 67 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
DB00368 9632 67 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
1028 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
139148732 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
479 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
5816 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
CHEMBL679 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
DB00668 7079 71 None -91 30 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
16731518 149060 0 None 26 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 628 9 4 5 2.5 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL388509 149060 0 None 26 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 628 9 4 5 2.5 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
228 7233 28 None -35 23 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
33 7233 28 None -35 23 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
6005 7233 28 None -35 23 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
CHEMBL53 7233 28 None -35 23 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
DB00714 7233 28 None -35 23 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
16732431 150809 0 None -34 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 735 11 4 7 3.3 CN1C[C@H](C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCCC(C(N)=O)C2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm060947x
CHEMBL390299 150809 0 None -34 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 735 11 4 7 3.3 CN1C[C@H](C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCCC(C(N)=O)C2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm060947x
16732899 175484 0 None - 1 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL436797 175484 0 None - 1 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
16731520 149129 0 None - 1 Human 5.1 pKd = 5.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL388732 149129 0 None - 1 Human 5.1 pKd = 5.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
5 6927 72 None -23442 53 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
5202 6927 72 None -23442 53 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
CHEMBL39 6927 72 None -23442 53 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
DB08839 6927 72 None -23442 53 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
4350931 176092 44 None 63 7 Rat 10.1 pKi = 10.1 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
CHEMBL441618 176092 44 None 63 7 Rat 10.1 pKi = 10.1 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
127026236 144896 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3763331 144896 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3765893 144896 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
3036864 209533 19 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL1256645 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL1814790 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL62 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
3036864 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1256645 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1814790 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL62 209533 19 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
3036864 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
3036864 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL1256645 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL1814790 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL62 209533 19 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
3036864 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL1256645 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL1814790 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL62 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
11465618 109175 23 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL3039528 109175 23 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL5191141 109175 23 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
3036864 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL1256645 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL1814790 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL62 209533 19 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
3036864 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 209533 19 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1256645 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1814790 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL62 209533 19 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
3036864 209533 19 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1256645 209533 19 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1814790 209533 19 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL62 209533 19 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
11154178 207005 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
CHEMBL596824 207005 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
162657549 187763 0 None 630 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 355 1 1 3 5.3 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4758723 187763 0 None 630 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 355 1 1 3 5.3 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
46231926 207358 0 None 12 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 207358 0 None 12 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231992 207422 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 389 1 1 2 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599528 207422 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 389 1 1 2 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 209533 19 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL1256645 209533 19 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL1814790 209533 19 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL62 209533 19 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
14896355 33606 0 None 10 3 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(Br)c2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL13632 33606 0 None 10 3 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(Br)c2)C1 10.1016/s0960-894x(00)00185-2
1243 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
944 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
CHEMBL324017 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
3038603 108642 8 None 2 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 108642 8 None 2 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
3036864 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1256645 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1814790 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL62 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
3036864 209533 19 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL1256645 209533 19 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL1814790 209533 19 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL62 209533 19 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
3036864 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL1256645 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL1814790 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL62 209533 19 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
11269330 208272 0 None 34 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 208272 0 None 34 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3039881 181036 10 None 4 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 181036 10 None 4 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
11558055 79927 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL1204122 79927 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL201170 79927 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
3036864 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
11558055 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL1204122 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201170 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
11558055 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL1204122 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
3036864 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1256645 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1814790 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL62 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
11558055 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
14787973 109444 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1cccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)c1 10.1021/jm00170a025
CHEMBL304535 109444 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1cccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)c1 10.1021/jm00170a025
3036864 209533 19 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1256645 209533 19 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1814790 209533 19 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL62 209533 19 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
3036864 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
11558055 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 79927 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
46231993 207186 0 None 562 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 407 1 1 2 5.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598104 207186 0 None 562 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 407 1 1 2 5.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL1256645 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL1814790 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL62 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
3036864 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
3036864 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL1256645 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL1814790 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL62 209533 19 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
3036864 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL1256645 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL1814790 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL62 209533 19 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
11595240 146966 0 None -5 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 146966 0 None -5 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
162655154 187552 0 None 204 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4756254 187552 0 None 204 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
44320357 213178 0 None 1202 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 213178 0 None 1202 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11235174 207160 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL597909 207160 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11374299 207387 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599282 207387 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
46231588 208040 0 None 12022 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 408 4 1 4 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL603901 208040 0 None 12022 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 408 4 1 4 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
3036864 209533 19 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL1256645 209533 19 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL1814790 209533 19 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL62 209533 19 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
44439943 100141 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245570 100141 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
11465618 109175 23 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 109175 23 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 109175 23 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
44439943 100141 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL245570 100141 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2008.04.081
86346162 139218 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 433 3 1 4 4.2 Cc1cc(Oc2ncccc2I)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697581 139218 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 433 3 1 4 4.2 Cc1cc(Oc2ncccc2I)ccc1-c1c(C)n[nH]c(=O)c1C nan
10088113 169056 6 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1744079 169056 6 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL416401 169056 6 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
11488247 207418 0 None 1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 207418 0 None 1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
46232135 207103 0 None 85 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 428 1 2 2 6.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc5[nH]ccc5c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597503 207103 0 None 85 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 428 1 2 2 6.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc5[nH]ccc5c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 207187 0 None 5 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 207187 0 None 5 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231784 208117 0 None 2 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 208117 0 None 2 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231995 208313 0 None 7 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 208313 0 None 7 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44268809 105041 0 None 46 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
CHEMBL274577 105041 0 None 46 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
24873463 154822 0 None 3467 2 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 557 10 0 5 6.0 O=C(CCCN1CCN2CC3C(CC2C1)c1ccccc1N3CCCC(=O)c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
CHEMBL393466 154822 0 None 3467 2 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 557 10 0 5 6.0 O=C(CCCN1CCN2CC3C(CC2C1)c1ccccc1N3CCCC(=O)c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
46231645 207130 0 None 776 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 518 6 1 3 7.2 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(Cc3ccccc3)c3ccc(F)cc3F)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL597702 207130 0 None 776 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 518 6 1 3 7.2 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(Cc3ccccc3)c3ccc(F)cc3F)cc2)C1 10.1016/j.bmcl.2009.12.100
46231709 207486 0 None 1548 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)Nc4c(Cl)cccc4Cl)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL599977 207486 0 None 1548 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)Nc4c(Cl)cccc4Cl)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11452916 207608 0 None 7 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600986 207608 0 None 7 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
44268693 30121 0 None 16 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2ccccc2Br)C1 10.1016/s0960-894x(00)00185-2
CHEMBL13325 30121 0 None 16 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2ccccc2Br)C1 10.1016/s0960-894x(00)00185-2
3036864 209533 19 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1256645 209533 19 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1814790 209533 19 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL62 209533 19 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
46232067 207068 0 None 16 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 2 1 3 5.7 CN(C)c1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL597310 207068 0 None 16 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 2 1 3 5.7 CN(C)c1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
46232066 208035 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 208035 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
46232134 208095 0 None 125 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 2 3 5.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc(CO)cc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604176 208095 0 None 125 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 2 3 5.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc(CO)cc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL1256645 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL1814790 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL62 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
3036864 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL1256645 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL1814790 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL62 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
10516818 32423 0 None 2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135197 32423 0 None 2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
14787971 176851 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccccc1[C@H]1CN(C)CCc2cc(Cl)c(O)cc21 10.1021/jm00170a025
CHEMBL444321 176851 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccccc1[C@H]1CN(C)CCc2cc(Cl)c(O)cc21 10.1021/jm00170a025
3036864 209533 19 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL1256645 209533 19 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL1814790 209533 19 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL62 209533 19 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
242 7258 124 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
34 7258 124 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
60795 7258 124 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
CHEMBL1112 7258 124 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
DB01238 7258 124 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
11681599 81948 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL203637 81948 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1016/j.bmcl.2008.04.081
44439942 158644 0 None 4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
CHEMBL396560 158644 0 None 4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
11681599 81948 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 81948 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
10802788 175017 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL433652 175017 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
10802788 175017 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL433652 175017 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
3036864 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1256645 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1814790 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL62 209533 19 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
46231541 206967 0 None 4 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL596622 206967 0 None 4 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
107930 8311 26 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
3304 8311 26 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
CHEMBL298406 8311 26 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
DB12273 8311 26 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
149506840 189927 0 None 120 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 371 1 1 3 5.8 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4795230 189927 0 None 120 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 371 1 1 3 5.8 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
46232065 207038 0 None 346 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 425 1 1 2 5.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cc(F)cc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597100 207038 0 None 346 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 425 1 1 2 5.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cc(F)cc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46216855 207157 0 None 2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 207157 0 None 2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
15111050 20120 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1192259 20120 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL543473 20120 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
130844 19974 14 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1191103 19974 14 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL543398 19974 14 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
71451380 88012 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 435 3 5 6 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1.O=C(O)/C(O)=C(/O)C(=O)O 10.1016/j.bmc.2012.08.058
CHEMBL2158641 88012 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 435 3 5 6 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1.O=C(O)/C(O)=C(/O)C(=O)O 10.1016/j.bmc.2012.08.058
6852376 98374 13 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL1467585 98374 13 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL24077 98374 13 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL503958 98374 13 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
167715 9651 14 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
969 9651 14 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL225230 9651 14 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
11393666 199765 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 199765 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 199765 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
46231927 208315 0 None 2 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 208315 0 None 2 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
13805900 50783 0 None -2 5 Bovine 9.0 pKi = 9.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@@H]1Cc2cccc(O)c2C[C@H]1C 10.1021/jm020990u
CHEMBL15136 50783 0 None -2 5 Bovine 9.0 pKi = 9.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@@H]1Cc2cccc(O)c2C[C@H]1C 10.1021/jm020990u
162646534 186362 0 None 123 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 362 1 1 4 5.0 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(C#N)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4742056 186362 0 None 123 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 362 1 1 4 5.0 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(C#N)cc32)CCN1C 10.1016/j.bmcl.2020.127563
1242 10385 27 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
935 10385 27 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
CHEMBL286080 10385 27 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
133538 10391 24 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
8443 10391 24 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
CHEMBL574558 10391 24 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
107930 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
5018 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
943 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
946 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
CHEMBL13668 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
107930 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 8311 26 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
15111051 20142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1192465 20142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL543704 20142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
13697621 20513 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1195188 20513 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL554009 20513 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
1153 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
12668023 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026874 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026875 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3341 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
6603851 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
933 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
939 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
985 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1160786 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1161520 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL588 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
DB00800 8409 58 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3036864 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
5018 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 10322 13 None 2 10 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
134139606 153126 0 None 288 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 419 3 2 5 3.9 CCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3921278 153126 0 None 288 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 419 3 2 5 3.9 CCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
3036864 209533 19 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1256645 209533 19 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1814790 209533 19 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL62 209533 19 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
10638646 32987 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135735 32987 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
11486421 207973 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL603485 207973 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
3036864 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL1256645 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL1814790 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL62 209533 19 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
142405815 187943 0 None -10 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 365 2 1 3 5.7 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4760903 187943 0 None -10 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 365 2 1 3 5.7 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
11223303 207609 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600987 207609 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
14787975 109009 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1 10.1021/jm00170a025
CHEMBL303012 109009 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1 10.1021/jm00170a025
162646218 186255 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4740880 186255 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
122324 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 6993 22 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
44415569 172713 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL425069 172713 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415569 172713 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 172713 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
46231849 208197 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 208197 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 209533 19 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL1256645 209533 19 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL1814790 209533 19 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL62 209533 19 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
129244 125449 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL2114388 125449 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL34170 125449 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
10638646 32987 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135735 32987 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
37461 23906 14 None -2 8 Rat 8.7 pKi = 8.7 Binding
Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/jm9911478
CHEMBL1255588 23906 14 None -2 8 Rat 8.7 pKi = 8.7 Binding
Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/jm9911478
46231925 208157 0 None 5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 208157 0 None 5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
73671785 136199 0 None - 1 Human 8.7 pKi = 8.7 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 3 2 6 2.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3671278 136199 0 None - 1 Human 8.7 pKi = 8.7 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 3 2 6 2.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
4350931 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL441618 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
10656804 123337 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL336366 123337 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
107930 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
3304 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
CHEMBL298406 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
DB12273 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
107930 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
3304 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
CHEMBL298406 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
DB12273 8311 26 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
4350931 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
4350931 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL441618 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
4350931 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 176092 44 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
12765746 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
12765746 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
9797664 173016 1 None -4 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 331 1 0 4 3.8 CN1CCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL426763 173016 1 None -4 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 331 1 0 4 3.8 CN1CCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
107930 8311 26 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
3304 8311 26 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
CHEMBL298406 8311 26 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
DB12273 8311 26 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
133538 10391 24 None -1 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
8443 10391 24 None -1 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
CHEMBL574558 10391 24 None -1 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
12765746 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL303313 109057 4 None -18 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
4106 9280 22 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
5358812 9280 22 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
89 9280 22 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
CHEMBL93240 9280 22 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
44348383 23075 0 None -10 2 Rat 8.7 pKi = 8.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1021/jm9706832
CHEMBL122536 23075 0 None -10 2 Rat 8.7 pKi = 8.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1021/jm9706832
135398745 9688 112 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 9688 112 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 9688 112 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 9688 112 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
15937726 171928 0 None 177 2 Rat 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 293 1 1 2 4.2 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL422796 171928 0 None 177 2 Rat 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 293 1 1 2 4.2 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
44579030 196460 0 None 10 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 377 7 0 3 5.7 CCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL515342 196460 0 None 10 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 377 7 0 3 5.7 CCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415558 86937 0 None 93 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4n3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213443 86937 0 None 93 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4n3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415657 175520 0 None 17 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 4 1 7 4.9 CCOc1csc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL437112 175520 0 None 17 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 4 1 7 4.9 CCOc1csc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
117773683 139220 0 None - 1 Human 8.0 pKi = 8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 403 5 1 6 3.5 Cc1cc(Oc2nccc(C)c2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697583 139220 0 None - 1 Human 8.0 pKi = 8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 403 5 1 6 3.5 Cc1cc(Oc2nccc(C)c2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
56594534 77375 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 77375 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
90140327 136190 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]c(C)c23)cc1 nan
CHEMBL3671269 136190 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]c(C)c23)cc1 nan
74223724 136195 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671274 136195 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223826 136215 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671293 136215 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
11637457 79862 1 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 79862 1 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
86764102 139256 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1ccnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)cc2)c1Cl nan
CHEMBL3697619 139256 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1ccnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)cc2)c1Cl nan
135398745 9688 112 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 9688 112 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 9688 112 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 9688 112 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
11271099 211436 0 None -501 4 Rat 7.0 pKi = 7 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 458 9 2 5 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(N)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL73665 211436 0 None -501 4 Rat 7.0 pKi = 7 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 458 9 2 5 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(N)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
15937722 122002 0 None - 1 Rat 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 294 1 1 3 3.1 CN1CCc2cc(Cl)c(O)cc2C(N2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL334650 122002 0 None - 1 Rat 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 294 1 1 3 3.1 CN1CCc2cc(Cl)c(O)cc2C(N2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
49782398 24224 0 None -138 5 Pig 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1257688 24224 0 None -138 5 Pig 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
6603820 102549 19 None 1 12 Rat 7.0 pKi = 7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL25856 102549 19 None 1 12 Rat 7.0 pKi = 7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
15711850 20011 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1191350 20011 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL542436 20011 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
242 7258 124 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 7258 124 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 7258 124 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 7258 124 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 7258 124 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
135398737 7745 93 None -44 90 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 7745 93 None -44 90 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 7745 93 None -44 90 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 7745 93 None -44 90 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 7745 93 None -44 90 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2337 10030 77 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 10030 77 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 10030 77 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 10030 77 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 10030 77 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
2389 10104 118 None -489 66 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 10104 118 None -489 66 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 10104 118 None -489 66 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 10104 118 None -489 66 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 10104 118 None -489 66 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
17449900 146320 13 None -3548 6 Pig 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 146320 13 None -3548 6 Pig 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
137633863 163404 0 None -436 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 163404 0 None -436 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44372154 60999 0 None -11 4 Bovine 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160749 60999 0 None -11 4 Bovine 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
9864676 134586 0 None -58 5 Bovine 6.0 pKi = 6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL366388 134586 0 None -58 5 Bovine 6.0 pKi = 6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
15115530 19690 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
CHEMBL1189085 19690 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
CHEMBL538023 19690 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
44339879 179061 0 None -186 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 179061 0 None -186 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
10357869 11656 0 None -158 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL104453 11656 0 None -158 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
44412458 146072 3 None -3090 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL379177 146072 3 None -3090 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
45112568 205585 0 None -229 3 Rat 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
CHEMBL583422 205585 0 None -229 3 Rat 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
145980271 173271 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 173271 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
145986752 174055 0 None -23 17 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 174055 0 None -23 17 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
10633305 42768 1 None -28 2 Bovine 4.0 pKi = 4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2ccc(C)cc2C)C1 10.1021/jm9708700
CHEMBL144302 42768 1 None -28 2 Bovine 4.0 pKi = 4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2ccc(C)cc2C)C1 10.1021/jm9708700
44329093 214491 0 None -309 3 Bovine 4.0 pKi = 4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@@H]1CCn2ccc(CO)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL95618 214491 0 None -309 3 Bovine 4.0 pKi = 4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@@H]1CCn2ccc(CO)c2C1 10.1016/s0960-894x(01)00564-9
44304814 209651 0 None -16 4 Bovine 4.0 pKi = 4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL62601 209651 0 None -16 4 Bovine 4.0 pKi = 4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
71109993 150025 0 None - 1 Human 6.0 pKi = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
CHEMBL3896617 150025 0 None - 1 Human 6.0 pKi = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
228 7233 28 None -4 23 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
33 7233 28 None -4 23 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
6005 7233 28 None -4 23 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
CHEMBL53 7233 28 None -4 23 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
DB00714 7233 28 None -4 23 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
228 7233 28 None -30 23 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
33 7233 28 None -30 23 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
6005 7233 28 None -30 23 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
CHEMBL53 7233 28 None -30 23 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
DB00714 7233 28 None -30 23 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
74223776 136210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1C#N nan
CHEMBL3671289 136210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1C#N nan
28417 46813 49 None -1 12 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -1 12 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
15711865 19947 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL1190906 19947 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL541838 19947 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
3246545 209253 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 209253 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 209253 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
44415394 148611 0 None 15 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 471 3 1 5 4.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)/C=C/c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL386424 148611 0 None 15 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 471 3 1 5 4.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)/C=C/c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
13864380 213211 1 None 4 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87958 213211 1 None 4 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
13864381 215123 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL542683 215123 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL99361 215123 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
10637496 119661 0 None -58 3 Rat 6.0 pKi = 6.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 2 0 2 4.0 CCc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL331005 119661 0 None -58 3 Rat 6.0 pKi = 6.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 2 0 2 4.0 CCc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
44405995 79771 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
CHEMBL200802 79771 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
56593482 10713 3 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 10713 3 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 10713 3 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
156018236 184691 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4645139 184691 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
154706030 183324 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 183324 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 183324 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
76325156 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
12050197 107651 0 None -79 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL293645 107651 0 None -79 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
10570422 171684 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 6 2 3 4.0 CNCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL422267 171684 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 6 2 3 4.0 CNCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
15627832 105310 0 None -6 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 345 0 2 3 3.6 CN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL276326 105310 0 None -6 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 345 0 2 3 3.6 CN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
13646434 131432 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743799 131432 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL36416 131432 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
70692652 82839 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057441 82839 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
72708059 98971 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425369 98971 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
161665 179364 35 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL448891 179364 35 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
1353 8692 93 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 8692 93 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 8692 93 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 8692 93 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 8692 93 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
72708059 98971 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425369 98971 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
45112462 203745 0 None -831 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
CHEMBL566533 203745 0 None -831 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
154706123 183067 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 183067 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 183067 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
11724078 48481 1 None -2 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cccnc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL149240 48481 1 None -2 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cccnc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
154706513 183365 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4440698 183365 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 183365 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
3117 214620 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44448066 101650 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL253948 101650 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 10.1021/jm060959i
154704141 183458 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4561808 183458 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598299 183458 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
117774721 139223 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 5 1 6 2.8 Cc1c(-c2ccc(Oc3ncccc3OC(F)F)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697586 139223 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 5 1 6 2.8 Cc1c(-c2ccc(Oc3ncccc3OC(F)F)cc2)n(C)c(=O)[nH]c1=O nan
112500032 139248 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697610 139248 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)cnc(=O)n1C nan
10333842 105207 1 None -50 8 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
CHEMBL27559 105207 1 None -50 8 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
76325156 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 113167 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
9951964 213137 0 None -22 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87458 213137 0 None -22 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm00042a009
44415644 148599 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 583 4 1 5 7.3 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4N(NC(=O)c4ccccc4Cl)c4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
CHEMBL386336 148599 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 583 4 1 5 7.3 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4N(NC(=O)c4ccccc4Cl)c4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
10490043 120498 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960189i
CHEMBL332332 120498 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960189i
44386623 67829 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 376 3 0 4 4.2 COc1c(Cl)c2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
CHEMBL176356 67829 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 376 3 0 4 4.2 COc1c(Cl)c2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
1212 8443 50 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44415633 86782 0 None 8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 7 5.1 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL212807 86782 0 None 8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 7 5.1 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
44415578 148281 0 None 57 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL384500 148281 0 None 57 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134151737 159753 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 5 2 5 3.9 CCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3975220 159753 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 5 2 5 3.9 CCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
127031424 145647 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 6 1 5 4.2 CCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3781840 145647 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 6 1 5 4.2 CCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
75201901 173204 19 None -1 24 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None -1 24 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
44370173 55259 1 None -18 2 Bovine 7.0 pKi = 7.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 331 6 2 4 4.0 CCCN(CCc1cccs1)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
CHEMBL155613 55259 1 None -18 2 Bovine 7.0 pKi = 7.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 331 6 2 4 4.0 CCCN(CCc1cccs1)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
75201901 173204 19 None -1 24 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -1 24 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
122189393 130026 0 None -20 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 130026 0 None -20 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
122189394 130027 0 None -354 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613880 130027 0 None -354 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
21302486 116577 0 None -117 4 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 379 5 1 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCN3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233143 116577 0 None -117 4 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 379 5 1 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCN3)c1ccc(F)cc1 10.1021/jm401958n
10092819 23545 0 None -1412 11 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 23545 0 None -1412 11 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
11133602 37548 0 None -63 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL139600 37548 0 None -63 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44276404 105854 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL28054 105854 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
44276557 106092 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL282136 106092 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
11761412 123729 0 None -2290 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 123729 0 None -2290 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
10490043 120498 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm060959i
CHEMBL332332 120498 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm060959i
71459761 90855 0 None -181 7 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 90855 0 None -181 7 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
137635685 162784 0 None -38 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 162784 0 None -38 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
25072633 166000 0 None -1584 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 166000 0 None -1584 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
118709166 120189 0 None -19 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318838 120189 0 None -19 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
164615845 191969 0 None -1 6 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
CHEMBL4857492 191969 0 None -1 6 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
10833953 37898 0 None -1445 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140006 37898 0 None -1445 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
44380697 64867 0 None -61 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167414 64867 0 None -61 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44380685 65509 0 None -77 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168566 65509 0 None -77 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44380815 65784 0 None -234 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169193 65784 0 None -234 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
44264682 104093 0 None -2754 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
CHEMBL269202 104093 0 None -2754 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
15508243 12075 22 None -7 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL106635 12075 22 None -7 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
25099153 194032 0 None -4073 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 436 9 2 5 4.7 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL492664 194032 0 None -4073 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 436 9 2 5 4.7 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
45270021 201943 0 None -158 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL550392 201943 0 None -158 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
45272580 203235 0 None -165 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563109 203235 0 None -165 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
102262219 146837 0 None -22908 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 146837 0 None -22908 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137655029 165725 0 None -2691 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4095881 165725 0 None -2691 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
137657427 166338 0 None -9772 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4102628 166338 0 None -9772 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
10361512 61213 0 None -4786 5 Bovine 5.0 pKi = 5.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 61213 0 None -4786 5 Bovine 5.0 pKi = 5.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
154706590 183088 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4590839 183088 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4595264 183088 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
71110301 98973 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425371 98973 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44415368 86378 0 None 17 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 465 4 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCC3CCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL211461 86378 0 None 17 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 465 4 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCC3CCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
14198586 208612 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL60706 208612 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1016/j.bmc.2009.05.079
156013666 184058 0 None -10 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 3 1 4 3.6 COc1cc2c3c(c1OC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636318 184058 0 None -10 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 3 1 4 3.6 COc1cc2c3c(c1OC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
2726 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
154704536 183226 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4467528 183226 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4596340 183226 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154703875 183227 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 183227 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 183227 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
11335419 73874 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 73874 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
74223726 136197 16 None - 1 Human 7.0 pKi = 7.0 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C 10.1021/acs.jmedchem.8b01767
CHEMBL3671276 136197 16 None - 1 Human 7.0 pKi = 7.0 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C 10.1021/acs.jmedchem.8b01767
74223726 136197 16 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671276 136197 16 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
10497993 175253 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL43514 175253 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
3038495 7495 37 None -616 18 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 7495 37 None -616 18 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 7495 37 None -616 18 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
136074293 209836 0 None -3 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1cnc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm00067a009
CHEMBL63590 209836 0 None -3 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1cnc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm00067a009
45481842 204840 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 3 1 2 3.8 CCCCC1c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
CHEMBL574112 204840 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 3 1 2 3.8 CCCCC1c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
56589561 77376 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 77376 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
135398737 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
38 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
722 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
CHEMBL42 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
DB00363 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
242 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
242 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 7258 124 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
76325154 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3115580 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3139475 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
154703647 183144 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4450429 183144 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 183144 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
135398737 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
38 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
722 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
CHEMBL42 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
DB00363 7745 93 None -83 90 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
156016177 184433 0 None -114 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
CHEMBL4641502 184433 0 None -114 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
12049520 107842 5 None -45 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL294780 107842 5 None -45 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
44593524 190835 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmc.2008.05.077
CHEMBL482276 190835 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmc.2008.05.077
76325154 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3115580 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3139475 113183 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
44448062 101623 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253737 101623 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
117774133 139196 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 5 4.1 Cc1cc(Oc2ncc(Cl)cc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697559 139196 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 5 4.1 Cc1cc(Oc2ncc(Cl)cc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90644065 118438 0 None -8 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3286429 118438 0 None -8 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
53318565 65375 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684134 65375 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
10000788 54767 0 None -41 3 Rat 5.9 pKi = 5.9 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 395 6 1 4 3.9 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCN(c3ccccc3OC)CC1)CC2 10.1016/0960-894X(95)00076-6
CHEMBL155006 54767 0 None -41 3 Rat 5.9 pKi = 5.9 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 395 6 1 4 3.9 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCN(c3ccccc3OC)CC1)CC2 10.1016/0960-894X(95)00076-6
10832461 58038 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)c2c(c1)CCN(C)C2Cc1ccccc1O 10.1021/jm991034o
CHEMBL158067 58038 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)c2c(c1)CCN(C)C2Cc1ccccc1O 10.1021/jm991034o
86763998 139252 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697614 139252 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
135398745 9688 112 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
47 9688 112 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
CHEMBL715 9688 112 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
DB00334 9688 112 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
91899760 136225 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 1 5 4.3 Cc1cc(Oc2nccc3n[nH]cc23)c(F)cc1-c1c(C)ncnc1C nan
CHEMBL3671302 136225 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 1 5 4.3 Cc1cc(Oc2nccc3n[nH]cc23)c(F)cc1-c1c(C)ncnc1C nan
12304090 94283 36 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334886 94283 36 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@H]21 10.1016/j.bmc.2012.12.016
135398745 9688 112 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
47 9688 112 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
CHEMBL715 9688 112 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
DB00334 9688 112 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
168289523 198278 0 None -5 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 198278 0 None -5 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
10276451 207064 37 None -3388 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 207064 37 None -3388 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 207064 37 None -3388 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
10531 8202 21 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
2435 10362 83 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 10362 83 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 10362 83 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 10362 83 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 10362 83 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
25141414 189260 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 5 0 3 4.9 CCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL478671 189260 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 5 0 3 4.9 CCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415721 86817 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 605 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212936 86817 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 605 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415703 86596 0 None 537 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)c(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212077 86596 0 None 537 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)c(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415688 86946 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213477 86946 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134143833 157294 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 355 4 2 5 3.6 CCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3954556 157294 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 355 4 2 5 3.6 CCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
127031403 145512 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 381 5 1 5 3.9 COc1cc2c(cc1O)C1Cc3ccc(OCC4CC4)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780184 145512 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 381 5 1 5 3.9 COc1cc2c(cc1O)C1Cc3ccc(OCC4CC4)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
10733562 153792 0 None 25 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL39266 153792 0 None 25 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
9819042 19929 3 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL1190761 19929 3 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL541559 19929 3 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
1241 106955 24 None -2 8 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL288090 106955 24 None -2 8 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL552611 106955 24 None -2 8 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
117773867 139232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 1 4 4.9 Cc1cc(Oc2nccc(C)c2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697594 139232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 1 4 4.9 Cc1cc(Oc2nccc(C)c2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
6917970 10463 61 None -1 33 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
8370 10463 61 None -1 33 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
CHEMBL487387 10463 61 None -1 33 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
127031422 145496 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 4 1 5 3.5 CCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3779928 145496 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 4 1 5 3.5 CCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
14198584 205048 0 None 12 2 Rat 7.9 pKi = 7.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00118a012
CHEMBL57579 205048 0 None 12 2 Rat 7.9 pKi = 7.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00118a012
117773559 139261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 416 3 2 5 3.7 Cc1c(-c2ccc(Oc3ncccc3C(F)(F)F)c3[nH]ccc23)n(C)c(=O)[nH]c1=O nan
CHEMBL3697624 139261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 416 3 2 5 3.7 Cc1c(-c2ccc(Oc3ncccc3C(F)(F)F)c3[nH]ccc23)n(C)c(=O)[nH]c1=O nan
10005244 118128 0 None 7 2 Rat 6.9 pKi = 6.9 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 476 5 1 3 5.9 CN(C)c1ccc(/C=C/CN2CCc3cc(Br)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL326927 118128 0 None 7 2 Rat 6.9 pKi = 6.9 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 476 5 1 3 5.9 CN(C)c1ccc(/C=C/CN2CCc3cc(Br)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44323876 213361 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL88870 213361 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
1353 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
117773696 139204 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 6 2.7 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1F nan
CHEMBL3697567 139204 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 6 2.7 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1F nan
86764101 139255 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
CHEMBL3697618 139255 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
276 10286 50 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 10286 50 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 10286 50 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
11575479 101518 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253096 101518 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
1353 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 8692 93 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
118709178 120125 0 None -69 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3317465 120125 0 None -69 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189392 130025 0 None -54 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 130025 0 None -54 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
71458071 86275 0 None -102 6 Bovine 5.9 pKi = 5.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 86275 0 None -102 6 Bovine 5.9 pKi = 5.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
6603820 102549 19 None -4 12 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9800292
CHEMBL25856 102549 19 None -4 12 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9800292
6603954 209384 2 None -81 3 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm9800292
CHEMBL612083 209384 2 None -81 3 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm9800292
11068912 37637 0 None -39 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL139722 37637 0 None -39 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
11057969 40045 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL141845 40045 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44360992 126182 0 None -134 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
CHEMBL344677 126182 0 None -134 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
11036640 127925 0 None -29 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL357684 127925 0 None -29 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44264642 211582 0 None -398 4 Bovine 5.9 pKi = 5.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7506 211582 0 None -398 4 Bovine 5.9 pKi = 5.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
56833463 75111 0 None -602 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916552 75111 0 None -602 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
137643951 165038 0 None -831 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 165038 0 None -831 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
56837635 76083 0 None -3981 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 76083 0 None -3981 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709164 120187 0 None -199 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318836 120187 0 None -199 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44371932 126426 0 None -467 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL346805 126426 0 None -467 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
10404144 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
10404144 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
CHEMBL7927 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
44380785 127581 0 None -363 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL355566 127581 0 None -363 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
10404144 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7927 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10404144 212081 23 None -2187 10 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
CHEMBL7927 212081 23 None -2187 10 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
44340097 16212 0 None -4365 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 16212 0 None -4365 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
45270861 201859 0 None -33 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL549638 201859 0 None -33 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
681 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
940 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
947 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
CHEMBL59 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
DB00988 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
137651322 164254 0 None -13489 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 164254 0 None -13489 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
137640189 163732 0 None -15848 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 163732 0 None -15848 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
681 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
940 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
947 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
CHEMBL59 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
DB00988 8247 72 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
107995 103901 20 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
29982233 103901 20 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
CHEMBL267723 103901 20 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
44329282 175894 0 None -19 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL440143 175894 0 None -19 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
10404144 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 212081 23 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10247720 19826 1 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 19826 1 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 19826 1 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10474964 137249 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 137249 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 137249 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
10404144 212081 23 None -4466 10 Human 4.9 pKi = 4.9 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL7927 212081 23 None -4466 10 Human 4.9 pKi = 4.9 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/acs.jmedchem.7b00151
45481841 204839 0 None -14 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(Cl)c(O)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574111 204839 0 None -14 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(Cl)c(O)cc21 10.1016/j.bmc.2009.05.079
90142280 174075 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4293757 174075 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
15711855 20184 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192799 20184 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL544099 20184 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
13838742 106177 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
CHEMBL282710 106177 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
117773223 139229 0 None - 1 Human 5.9 pKi = 5.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 350 4 2 5 2.6 Cc1cc(Oc2ncccc2C(N)=O)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697591 139229 0 None - 1 Human 5.9 pKi = 5.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 350 4 2 5 2.6 Cc1cc(Oc2ncccc2C(N)=O)ccc1-c1c(C)n[nH]c(=O)c1C nan
25129807 110071 0 None -63 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084502 110071 0 None -63 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
91899762 136230 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cn[nH]c(=O)c1C nan
CHEMBL3671307 136230 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cn[nH]c(=O)c1C nan
491 6980 9 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 6980 9 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 6980 9 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
2284 9956 33 None -36 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 9956 33 None -36 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 9956 33 None -36 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 9956 33 None -36 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 9956 33 None -36 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44415582 145768 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 444 1 0 4 5.3 Cc1ccccc1C(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL378543 145768 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 444 1 0 4 5.3 Cc1ccccc1C(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
681 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
940 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
947 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
CHEMBL59 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
DB00988 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
44241581 20793 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197218 20793 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL562935 20793 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
3032727 20248 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL1193245 20248 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL544618 20248 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
74223828 136221 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 4 1 6 3.8 COc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671299 136221 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 4 1 6 3.8 COc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
10519436 17998 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1178784 17998 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL41238 17998 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
10664137 169534 0 None 10 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL417164 169534 0 None 10 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
15711851 20312 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL1193797 20312 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL545264 20312 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
9838572 70227 0 None -23 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 279 1 0 3 2.6 CN1CCN(C2=Cc3ccccc3Cn3cccc32)CC1 10.1021/jm049629t
CHEMBL179775 70227 0 None -23 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 279 1 0 3 2.6 CN1CCN(C2=Cc3ccccc3Cn3cccc32)CC1 10.1021/jm049629t
10072800 103437 4 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL263790 103437 4 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL554199 103437 4 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
12050193 209975 0 None -2 4 Bovine 5.9 pKi = 5.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64325 209975 0 None -2 4 Bovine 5.9 pKi = 5.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
12050199 107589 0 None -32 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL293225 107589 0 None -32 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
10068602 106979 1 None -4677 3 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 384 6 0 4 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28831 106979 1 None -4677 3 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 384 6 0 4 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
71528209 93747 0 None -1949 7 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 93747 0 None -1949 7 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
57398351 76933 0 None -13 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 76933 0 None -13 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
10801923 184543 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4642805 184543 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
44555445 206708 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)Cc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL594789 206708 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)Cc1ccccc1C2 10.1016/j.bmc.2009.08.028
127027739 144762 0 None -11220 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 382 7 1 6 1.7 O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3764390 144762 0 None -11220 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 382 7 1 6 1.7 O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
60167166 82070 0 None -41 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037430 82070 0 None -41 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
441383 27105 57 None -12 17 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -12 17 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
154705038 183425 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4584481 183425 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 183425 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
145967904 171876 0 None -11 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 171876 0 None -11 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145988180 172010 0 None -10 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 172010 0 None -10 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
72699716 121967 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344459 121967 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
44326751 115392 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL320572 115392 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL539544 115392 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
24949690 188385 0 None -1819 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
CHEMBL477200 188385 0 None -1819 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
154705015 183293 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 183293 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 183293 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4576555 220796 5 None -1 19 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D1GPCRScan assay: inhibition of D1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
9930475 213069 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87026 213069 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm981094e
9930475 213069 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87026 213069 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm00042a009
91899761 136227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 317 3 1 5 3.8 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
CHEMBL3671304 136227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 317 3 1 5 3.8 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
15937725 123883 0 None 158 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 279 1 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C(C2CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL339342 123883 0 None 158 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 279 1 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C(C2CCCC2)C1 10.1016/S0960-894X(00)80155-9
44415615 146313 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL379560 146313 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415507 87062 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL214016 87062 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
10710466 163194 0 None 11 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL40667 163194 0 None 11 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
74223725 136196 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671275 136196 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C nan
117774412 139233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.5 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)F nan
CHEMBL3697595 139233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.5 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)F nan
44281202 107181 3 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 379 1 1 2 3.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL290118 107181 3 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 379 1 1 2 3.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
44320061 112809 0 None 75 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313304 112809 0 None 75 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
17755866 149662 1 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 149662 1 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
681 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
940 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
947 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
CHEMBL59 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
DB00988 8247 72 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
15115517 16485 0 None -426 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL113196 16485 0 None -426 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
6852376 98374 13 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL1467585 98374 13 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL24077 98374 13 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL503958 98374 13 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
2865 10915 73 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 10915 73 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 10915 73 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 10915 73 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 10915 73 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
146025727 178464 0 None -4 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None -4 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44415686 86754 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 7 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212700 86754 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 7 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
24800527 162499 0 None -4 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 1 3 3.5 CCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL405369 162499 0 None -4 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 1 3 3.5 CCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
57403525 76929 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 76929 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
118709159 120182 0 None -21 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318831 120182 0 None -21 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
2337 10030 77 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 10030 77 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 10030 77 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 10030 77 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 10030 77 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
44403219 78679 0 None -1174 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
CHEMBL197162 78679 0 None -1174 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
10448562 121898 1 None 12 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 121898 1 None 12 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
16105549 74560 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL1908879 74560 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL221640 74560 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
71459759 90846 0 None -81 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207633 90846 0 None -81 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44567686 198846 0 None -1 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 265 1 0 2 3.4 COc1cc2c3c(c1)-c1ccccc1C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.06.016
CHEMBL520262 198846 0 None -1 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 265 1 0 2 3.4 COc1cc2c3c(c1)-c1ccccc1C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.06.016
53327663 73253 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852239 73253 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3215641 73253 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
137643309 165194 0 None -1174 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 165194 0 None -1174 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
122181326 128645 0 None -426 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 128645 0 None -426 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
122181329 128648 0 None -4168 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 128648 0 None -4168 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
57402787 75970 0 None -371 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 75970 0 None -371 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
9995904 37993 4 None -14454 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL140099 37993 4 None -14454 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
11626748 146937 0 None -14 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
CHEMBL380287 146937 0 None -14 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
44340186 16432 0 None -45 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 16432 0 None -45 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
9995904 37993 4 None -14454 5 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 37993 4 None -14454 5 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
25139180 191120 0 None -42 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL484357 191120 0 None -42 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
25099152 194065 0 None -38 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 466 9 2 5 5.1 CCCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c2ccccc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL492883 194065 0 None -38 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 466 9 2 5 5.1 CCCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c2ccccc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
25130817 194291 0 None -37 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 518 9 2 5 6.5 CC(C)CCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494309 194291 0 None -37 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 518 9 2 5 6.5 CC(C)CCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
73347474 97834 0 None -12882 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397478 97834 0 None -12882 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
137655556 165318 0 None -3801 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4091507 165318 0 None -3801 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
71733935 97758 0 None -30902 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 97758 0 None -30902 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
14665503 98009 0 None -21379 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL240106 98009 0 None -21379 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
44437896 159247 0 None -1174 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397103 159247 0 None -1174 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
44329283 214420 0 None -30 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@H]1CCn2c(CO)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL95230 214420 0 None -30 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@H]1CCn2c(CO)ccc2C1 10.1016/s0960-894x(01)00564-9
53321194 65376 0 None -56 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684135 65376 0 None -56 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
154724650 183116 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4543870 183116 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 183116 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
154706711 183294 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4439535 183294 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596930 183294 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
10024430 214392 0 None -41 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL95098 214392 0 None -41 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
135398737 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
38 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
722 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
CHEMBL42 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
DB00363 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
135398737 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
38 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
722 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
CHEMBL42 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
DB00363 7745 93 None -44 90 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
156011597 184158 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4637938 184158 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
72699717 121968 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 5 1 4 4.9 CCCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344460 121968 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 5 1 4 4.9 CCCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
2600 10551 74 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 10551 74 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 10551 74 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 10551 74 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 10551 74 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
57393083 76942 0 None -21 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 76942 0 None -21 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
45483261 204665 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 380 3 0 6 3.4 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2ncncc21 10.1016/j.bmcl.2009.09.041
CHEMBL572708 204665 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 380 3 0 6 3.4 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2ncncc21 10.1016/j.bmcl.2009.09.041
11795165 16141 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL111352 16141 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL541842 16141 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
45267373 20790 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197201 20790 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL562460 20790 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
44278589 105226 0 None -11 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@@H]1Cc1ccccc1-3 10.1021/jm00402a024
CHEMBL27574 105226 0 None -11 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@@H]1Cc1ccccc1-3 10.1021/jm00402a024
5311191 119408 7 None -35 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL330274 119408 7 None -35 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
15021875 111146 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm00111a046
CHEMBL310153 111146 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm00111a046
15021875 111146 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm981094e
CHEMBL310153 111146 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm981094e
10645469 117334 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL325253 117334 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL542428 117334 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
9979654 214698 0 None -14 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL96781 214698 0 None -14 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
155516042 183072 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 183072 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 183072 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
12442999 94285 6 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334890 94285 6 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
57391307 76938 0 None -19 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 76938 0 None -19 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
71722301 109250 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3040157 109250 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3216146 109250 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
53324045 63845 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 63845 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
44358192 208922 5 None -676 2 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 345 1 2 2 2.3 CN1C[C@H](C(N)=O)C=C2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1021/jm9800292
CHEMBL609151 208922 5 None -676 2 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 345 1 2 2 2.3 CN1C[C@H](C(N)=O)C=C2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1021/jm9800292
10862670 25274 0 None -281 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL126439 25274 0 None -281 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL127317 25274 0 None -281 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
15467373 108631 0 None -107 4 Bovine 4.9 pKi = 4.9 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL300553 108631 0 None -107 4 Bovine 4.9 pKi = 4.9 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
53946795 74507 1 None -1122 2 Rat 4.9 pKi = 4.9 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
CHEMBL1907814 74507 1 None -1122 2 Rat 4.9 pKi = 4.9 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
136074292 210349 0 None -3 2 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cnccc3Nc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL66730 210349 0 None -3 2 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cnccc3Nc3ccccc32)CC1 10.1021/jm00067a009
44304652 207101 0 None -28 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 207101 0 None -28 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
71062646 156322 0 None -2238 13 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 156322 0 None -2238 13 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
13373172 206562 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 206562 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
17756212 93143 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 93143 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
2286 9957 51 None -30 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 9957 51 None -30 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 9957 51 None -30 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 9957 51 None -30 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 9957 51 None -30 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
11080 35858 79 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 35858 79 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
44210226 123309 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
CHEMBL336218 123309 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
117773821 139239 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 1 4 4.0 Cc1cc(Oc2ncc(F)cc2C)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697601 139239 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 1 4 4.0 Cc1cc(Oc2ncc(F)cc2C)ccc1-c1c(C)n[nH]c(=O)c1C nan
10851717 85252 1 None -15 4 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 85252 1 None -15 4 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
154725484 183244 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 183244 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 183244 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
9970201 177422 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
CHEMBL445129 177422 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
168295528 199810 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
10249506 15577 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL109673 15577 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL544091 15577 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
10851717 85252 1 None -15 4 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 85252 1 None -15 4 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
155770281 184526 0 None -1 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 184526 0 None -1 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
23656544 176890 0 None -575 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 2 3 2.6 CN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL444368 176890 0 None -575 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 2 3 2.6 CN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
5352624 74013 44 None -3 5 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
CHEMBL18797 74013 44 None -3 5 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
2662 18156 131 None -3 30 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 18156 131 None -3 30 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
16104 168696 19 None -1 5 Rat 7.9 pKi = 7.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL415300 168696 19 None -1 5 Rat 7.9 pKi = 7.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
44415544 87012 0 None 169 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Br)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213775 87012 0 None 169 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Br)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415628 146570 0 None 104 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL379874 146570 0 None 104 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
156017431 184556 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643069 184556 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
10981731 22041 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL121274 22041 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
11014679 121566 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL333955 121566 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
16351 109507 47 None -4 6 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL304902 109507 47 None -4 6 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
9841398 106295 4 None 3 4 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL28338 106295 4 None 3 4 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
44320024 113844 0 None 51 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315750 113844 0 None 51 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86767093 136201 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
CHEMBL3671280 136201 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
16351 109507 47 None -4 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL304902 109507 47 None -4 6 Rat 7.9 pKi = 7.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
11014679 121566 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL333955 121566 0 None -3 2 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
10981731 22041 0 None -3 2 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL121274 22041 0 None -3 2 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
44276412 104441 0 None 10 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL27117 104441 0 None 10 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276556 106478 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL284644 106478 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
45482180 204683 0 None -17 4 Pig 6.9 pKi = 6.9 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL572867 204683 0 None -17 4 Pig 6.9 pKi = 6.9 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
130442480 182049 0 None -1 24 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -1 24 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
53328903 73232 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1802237 73232 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1852107 73232 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
52919 21222 48 None -15 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL1200986 21222 48 None -15 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
14198590 210165 1 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00118a012
CHEMBL65397 210165 1 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00118a012
10895106 39001 0 None -27 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL140968 39001 0 None -27 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10053476 123524 0 None -2570 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
CHEMBL337531 123524 0 None -2570 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
44454707 104607 0 None -28 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL272073 104607 0 None -28 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44393411 72867 0 None -316 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL183871 72867 0 None -316 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
71459760 90847 0 None -74 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207634 90847 0 None -74 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
25072941 163253 0 None -331 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 163253 0 None -331 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137640371 163593 0 None -933 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 163593 0 None -933 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
118709165 120188 0 None -66 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318837 120188 0 None -66 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709167 120190 0 None -16 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318839 120190 0 None -16 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709170 120194 0 None -53 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318842 120194 0 None -53 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44372296 126265 0 None -72 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL345357 126265 0 None -72 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL5074765 221111 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5079653 221410 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3NC4=O)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5085145 221730 0 None -4 2 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None N[C@H]1C[C@@H](CO)[C@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
CHEMBL5087121 221849 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None CN(C)C(=O)COC(=O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
44380774 127253 0 None -851 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL354180 127253 0 None -851 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
44336571 11603 0 None -61 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL104201 11603 0 None -61 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
15508239 13028 0 None -5 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL108160 13028 0 None -5 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
15508240 117304 0 None -15 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL325104 117304 0 None -15 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10496727 20034 0 None -24 3 Rat 4.9 pKi = 4.9 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 331 2 0 3 4.7 COc1c(-c2ccco2)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL119150 20034 0 None -24 3 Rat 4.9 pKi = 4.9 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 331 2 0 3 4.7 COc1c(-c2ccco2)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
90644066 118817 0 None -17 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289653 118817 0 None -17 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
53328721 73209 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1851968 73209 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216523 73209 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
279 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
49381 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
CHEMBL63756 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
279 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
49381 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
CHEMBL63756 8442 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
44210226 123309 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
CHEMBL336218 123309 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
14198588 178286 2 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 178286 2 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
14198590 210165 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00129a006
CHEMBL65397 210165 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00129a006
44582676 196558 0 None -10 17 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 196558 0 None -10 17 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
13922235 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
CHEMBL283489 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
13922235 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL283489 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
13922235 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL283489 106316 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
10433336 85293 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 439 8 1 4 4.3 BC#N.CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL2111925 85293 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 439 8 1 4 4.3 BC#N.CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
135 9310 43 None -46 56 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
1796 9310 43 None -46 56 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
4184 9310 43 None -46 56 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
CHEMBL6437 9310 43 None -46 56 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
DB06148 9310 43 None -46 56 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
5320227 102612 59 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 354 6 1 5 4.6 CC(C)=CC(O)C/C(C)=C/COc1c2ccoc2cc2oc(=O)ccc12 10.1016/j.bmc.2007.12.021
CHEMBL258939 102612 59 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 354 6 1 5 4.6 CC(C)=CC(O)C/C(C)=C/COc1c2ccoc2cc2oc(=O)ccc12 10.1016/j.bmc.2007.12.021
154706461 183127 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4470439 183127 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 183127 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
44537925 205523 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 205523 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
156010755 183920 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4633950 183920 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
11112574 25279 0 None -17 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 419 8 1 6 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL127344 25279 0 None -17 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 419 8 1 6 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3n2)CC1 10.1021/jm0211220
10732337 119768 0 None -13 3 Rat 5.8 pKi = 5.8 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 291 2 0 2 4.1 C=Cc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL331100 119768 0 None -13 3 Rat 5.8 pKi = 5.8 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 291 2 0 2 4.1 C=Cc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
70684207 82845 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057452 82845 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70684207 82845 0 None - 1 Human 5.8 pKi = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057452 82845 0 None - 1 Human 5.8 pKi = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
31101 7516 40 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 7516 40 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 7516 40 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 7516 40 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 7516 40 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
44582490 196916 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 4.2 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL517349 196916 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 4.2 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
1353 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
3559 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
86 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
CHEMBL54 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
DB00502 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
196129 74573 17 None -1819 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 74573 17 None -1819 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
154704368 183250 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4569006 183250 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 183250 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
11408148 135498 0 None -371 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 135498 0 None -371 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
154725234 183071 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4585289 183071 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 183071 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
73453 36389 24 None -208 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 36389 24 None -208 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
33630 185736 99 None -5 28 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 185736 99 None -5 28 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
2389 10104 118 None -346 66 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
5073 10104 118 None -346 66 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
96 10104 118 None -346 66 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
CHEMBL85 10104 118 None -346 66 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
DB00734 10104 118 None -346 66 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
156014482 183991 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635423 183991 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
2389 10104 118 None -489 66 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
5073 10104 118 None -489 66 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
96 10104 118 None -489 66 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
CHEMBL85 10104 118 None -489 66 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
DB00734 10104 118 None -489 66 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
21589014 150850 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3903297 150850 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
10044334 213900 18 None -64 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL92145 213900 18 None -64 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
44415568 146921 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL380236 146921 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
155529453 178217 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranesDisplacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranes
ChEMBL 385 4 2 3 4.3 COc1ccc2[nH]cc(C3=CCN(Cc4cc(=O)[nH]c5ccccc45)CC3)c2c1 10.1016/j.ejmech.2019.07.050
CHEMBL4463034 178217 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranesDisplacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranes
ChEMBL 385 4 2 3 4.3 COc1ccc2[nH]cc(C3=CCN(Cc4cc(=O)[nH]c5ccccc45)CC3)c2c1 10.1016/j.ejmech.2019.07.050
11406143 72906 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
CHEMBL184073 72906 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
10895039 25292 0 None -1000 7 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL127400 25292 0 None -1000 7 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL129022 25292 0 None -1000 7 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
44593524 190835 0 None -12 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.11.025
CHEMBL482276 190835 0 None -12 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.11.025
10740666 32895 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 416 6 1 3 4.5 CN(C)CCCCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL135616 32895 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 416 6 1 3 4.5 CN(C)CCCCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL4576555 220796 5 None -1 19 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of D1GPCRScan assay: inhibition of D1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
CHEMBL4576555 220796 5 None -1 19 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a DRD1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL5212743
117773324 139209 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2cc(C3CC3)ccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697572 139209 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2cc(C3CC3)ccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
1218 10388 30 None -11 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 10388 30 None -11 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 10388 30 None -11 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
44415611 173038 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 435 2 1 6 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccco3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL426868 173038 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 435 2 1 6 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccco3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11567963 161834 0 None 40 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 419 3 1 5 3.9 COc1cc2c(cc1OC)-c1c(OC)c(O)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401689 161834 0 None 40 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 419 3 1 5 3.9 COc1cc2c(cc1OC)-c1c(OC)c(O)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
10220 145538 16 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)C1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780481 145538 16 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)C1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
86763997 139251 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697613 139251 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
9884087 21409 0 None -4 2 Rat 7.8 pKi = 7.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.8 pKi = 7.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
86767098 136208 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671287 136208 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
130442572 178687 0 None -3 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -3 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44415395 144939 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 423 2 1 5 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL376928 144939 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 423 2 1 5 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
53328901 73255 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1802236 73255 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852245 73255 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
90644226 118556 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 118556 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709179 120203 0 None -61 4 Pig 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318851 120203 0 None -61 4 Pig 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
681 8247 72 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
940 8247 72 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
947 8247 72 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
CHEMBL59 8247 72 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
DB00988 8247 72 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
10546131 107185 0 None 20 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290149 107185 0 None 20 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
10476504 40261 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 40261 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44361021 125564 0 None -537 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
CHEMBL342060 125564 0 None -537 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
10884046 172148 0 None -107 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL423735 172148 0 None -107 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44436602 151991 0 None -245 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL391256 151991 0 None -245 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
44436598 156074 0 None -3388 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL394473 156074 0 None -3388 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
53361302 70624 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1803049 70624 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
11696910 84522 0 None -1174 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
CHEMBL209034 84522 0 None -1174 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
53361302 70624 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803049 70624 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
45268292 203466 0 None -446 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL564688 203466 0 None -446 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
71583848 94506 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 94506 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
137636498 162975 0 None -660 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 162975 0 None -660 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
118709171 120195 0 None -5 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318843 120195 0 None -5 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189389 130022 0 None -346 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 130022 0 None -346 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
13678304 108490 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 229 3 3 3 2.3 NCCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
CHEMBL299511 108490 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 229 3 3 3 2.3 NCCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
44371996 60397 0 None -8 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL160266 60397 0 None -8 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
44371980 60709 0 None -57 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160536 60709 0 None -57 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
44400674 131967 0 None -3019 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 131967 0 None -3019 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
44264623 211792 0 None -1174 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7686 211792 0 None -1174 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
11659604 145352 0 None -30 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL377542 145352 0 None -30 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
44336552 118117 1 None -53 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL326864 118117 1 None -53 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
9977478 211722 2 None -234422 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL76402 211722 2 None -234422 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
56926586 75784 0 None -2089 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923415 75784 0 None -2089 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44381217 65920 0 None -9 4 Bovine 4.8 pKi = 4.8 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL169889 65920 0 None -9 4 Bovine 4.8 pKi = 4.8 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
44371997 56704 0 None -10000 4 Bovine 4.8 pKi = 4.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
CHEMBL156851 56704 0 None -10000 4 Bovine 4.8 pKi = 4.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
154704941 183406 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4578364 183406 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597877 183406 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
167715 9651 14 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
969 9651 14 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
CHEMBL225230 9651 14 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
46231834 207691 0 None -117 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 488 3 1 5 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCN(c5ccccn5)CC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL601635 207691 0 None -117 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 488 3 1 5 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCN(c5ccccn5)CC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
10684714 107086 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 107086 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 107086 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL5289958 201265 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in HEK293 cell membrane assessed as inhibition constantDisplacement of [3H]SCH23390 from D1 receptor in HEK293 cell membrane assessed as inhibition constant
ChEMBL 429 4 1 2 5.6 Fc1ccc(CN2CCCC3(CCN(Cc4cc5ccc(Cl)cc5[nH]4)C3)C2)cc1F 10.1016/j.ejmech.2022.114840
72301 192897 76 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL487182 192897 76 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
44415367 86723 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 411 3 1 5 3.9 CCCC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL212597 86723 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 411 3 1 5 3.9 CCCC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
44401105 76351 0 None -17 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193435 76351 0 None -17 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
44320327 170203 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 170203 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10623632 55068 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 453 4 1 3 5.1 CCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
CHEMBL155351 55068 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 453 4 1 3 5.1 CCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
44326982 15431 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
CHEMBL109548 15431 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
CHEMBL545727 15431 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
9886130 213209 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87943 213209 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
9886130 213209 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87943 213209 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm00042a009
131990 50719 11 None -6 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cnccc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL151263 50719 11 None -6 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cnccc3Sc3ccccc32)CC1 10.1021/jm00030a011
156018868 184706 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 378 5 1 4 4.0 C=CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4645375 184706 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 378 5 1 4 4.0 C=CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
12050195 210063 0 None -21 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64696 210063 0 None -21 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
11057 182928 23 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 182928 23 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 182928 23 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 182928 23 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
117772791 139200 0 None - 1 Human 6.8 pKi = 6.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 323 3 1 5 2.5 Cc1cc(Oc2ccccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697563 139200 0 None - 1 Human 6.8 pKi = 6.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 323 3 1 5 2.5 Cc1cc(Oc2ccccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415625 86870 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213145 86870 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
11732785 170499 0 None -323 5 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
CHEMBL420510 170499 0 None -323 5 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
44278409 107110 0 None -616 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 418 6 0 4 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28946 107110 0 None -616 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 418 6 0 4 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
44415543 86725 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212608 86725 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415543 86725 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212608 86725 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
10052433 172136 0 None -501 4 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 521 10 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL423671 172136 0 None -501 4 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 521 10 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
16090821 88608 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL216439 88608 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
10851717 85252 1 None -15 4 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 85252 1 None -15 4 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
1353 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
3559 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
86 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
CHEMBL54 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
DB00502 8692 93 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
9817779 121210 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
CHEMBL333246 121210 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
1830 9368 44 None -16 28 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
207 9368 44 None -16 28 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
23897 9368 44 None -16 28 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
CHEMBL460 9368 44 None -16 28 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
DB01618 9368 44 None -16 28 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
10851717 85252 1 None -15 4 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 85252 1 None -15 4 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
44323894 174879 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL432762 174879 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
15115524 115787 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 735 3 5 8 7.8 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N/C(S)=N/c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)cc2)C1 10.1021/jm00115a012
CHEMBL321223 115787 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 735 3 5 8 7.8 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N/C(S)=N/c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)cc2)C1 10.1021/jm00115a012
6761 74574 19 None -5 18 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 74574 19 None -5 18 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44415701 86861 0 None 16 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 569 5 1 8 5.1 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL213110 86861 0 None 16 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 569 5 1 8 5.1 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
44415584 145472 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Br)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL377877 145472 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Br)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415601 148239 0 None 33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 481 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL384269 148239 0 None 33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 481 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
156018764 184574 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643426 184574 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
9844271 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL368324 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 21409 0 None -4 2 Rat 7.8 pKi = 7.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.8 pKi = 7.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
9844271 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL368324 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9844271 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL368324 137460 1 None 1 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
11716449 147993 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 147993 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
72699815 121974 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 349 3 1 4 3.9 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344467 121974 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 349 3 1 4 3.9 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
117773776 139237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 3 1 5 3.9 Cc1cc(Sc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697599 139237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 3 1 5 3.9 Cc1cc(Sc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
9817779 121210 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
CHEMBL333246 121210 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
45269168 202709 0 None -10 4 Bovine 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL559399 202709 0 None -10 4 Bovine 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
122189390 130023 0 None -16 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 130023 0 None -16 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
10973768 114337 0 None -4073 10 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 114337 0 None -4073 10 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
681 8247 72 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
10403608 84935 5 None -1584 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210405 84935 5 None -1584 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44412468 172709 0 None -616 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL425057 172709 0 None -616 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
53317282 65372 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684131 65372 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
24949534 196297 0 None -2041 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
CHEMBL514074 196297 0 None -2041 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
10403608 84935 5 None -1584 6 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL210405 84935 5 None -1584 6 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
145979897 173385 0 None -158 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4280542 173385 0 None -158 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
57400556 76085 0 None -2398 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 76085 0 None -2398 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
10476504 40261 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 40261 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
10824155 64014 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL165022 64014 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44436601 98718 0 None -1584 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL241424 98718 0 None -1584 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
15508238 11567 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
CHEMBL104092 11567 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
72544787 99905 0 None -501 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 99905 0 None -501 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
57400562 76093 0 None -16 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 76093 0 None -16 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
71449034 85198 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111526 85198 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44319361 212499 0 None -7 4 Bovine 4.8 pKi = 4.8 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 212499 0 None -7 4 Bovine 4.8 pKi = 4.8 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
10200496 90368 0 None -295 5 Human 6.8 pKi = 6.8 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 90368 0 None -295 5 Human 6.8 pKi = 6.8 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
11653679 187970 1 None -24 11 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 187970 1 None -24 11 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9872676 84970 0 None -4073 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None -4073 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
11419055 136082 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 431 4 1 5 3.0 O=C1NCCN1CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL367087 136082 0 None -12 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 431 4 1 5 3.0 O=C1NCCN1CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
10335576 127709 5 None 2 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3ccccc3Sc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL356076 127709 5 None 2 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3ccccc3Sc3ncccc32)CC1 10.1021/jm00030a011
44278267 107040 0 None -53 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 368 6 0 2 4.6 O=C1c2ccccc2CN1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28884 107040 0 None -53 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 368 6 0 2 4.6 O=C1c2ccccc2CN1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
16090821 88608 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 88608 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
46889212 14241 0 None -263 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccncc1 10.1016/j.bmcl.2010.02.106
CHEMBL1086958 14241 0 None -263 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccncc1 10.1016/j.bmcl.2010.02.106
13678338 107498 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.8 Oc1ccc(-c2c(O)c(O)c(Cl)c3c2CCNCC3)cc1 10.1021/jm00160a018
CHEMBL292611 107498 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.8 Oc1ccc(-c2c(O)c(O)c(Cl)c3c2CCNCC3)cc1 10.1021/jm00160a018
14198580 204741 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 301 3 0 2 4.1 COc1cc2c(cc1Cl)CCN(C)C2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL573412 204741 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 301 3 0 2 4.1 COc1cc2c(cc1Cl)CCN(C)C2Cc1ccccc1 10.1016/j.bmc.2009.05.079
154725766 183424 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4527244 183424 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4598000 183424 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10546132 168034 0 None 9 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL41196 168034 0 None 9 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
44299852 204914 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 245 3 4 4 2.0 NCCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
CHEMBL57470 204914 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 245 3 4 4 2.0 NCCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
11346967 132205 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 3 3.4 O=C(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
CHEMBL364586 132205 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 3 3.4 O=C(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
11812345 23685 0 None -5 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL125193 23685 0 None -5 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1cc2ccccc2o1 10.1021/jm0211220
15711860 20630 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1195937 20630 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL555619 20630 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
15069443 107748 0 None 3 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@H]21 10.1021/jm00128a038
CHEMBL294215 107748 0 None 3 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@H]21 10.1021/jm00128a038
154726922 183320 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442936 183320 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597157 183320 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
15696481 86441 0 None 21 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 86441 0 None 21 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
11404156 73056 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 311 6 0 3 3.4 CC1CN(CCOc2ccccc2Cc2ccccc2)CCO1 10.1021/jm049720x
CHEMBL184724 73056 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 311 6 0 3 3.4 CC1CN(CCOc2ccccc2Cc2ccccc2)CCO1 10.1021/jm049720x
71722295 109244 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397381 109244 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040115 109244 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
145990190 173632 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4285528 173632 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
127035062 143229 0 None -58 19 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 143229 0 None -58 19 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
135398737 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
38 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
722 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
CHEMBL42 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
DB00363 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
135398737 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
38 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
722 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
CHEMBL42 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
DB00363 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
24800688 162497 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 309 3 1 3 3.9 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL405345 162497 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 309 3 1 3 3.9 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
10498848 126830 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)cc2c1C(Cc1ccccc1O)N(C)CC2 10.1021/jm991034o
CHEMBL350471 126830 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)cc2c1C(Cc1ccccc1O)N(C)CC2 10.1021/jm991034o
72708061 98974 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425372 98974 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
44582461 188696 0 None 4 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 350 5 0 4 2.3 O=C1c2ccccc2CCN1CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477961 188696 0 None 4 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 350 5 0 4 2.3 O=C1c2ccccc2CCN1CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
70692655 82849 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057456 82849 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
71109804 94281 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 nan
CHEMBL2334882 94281 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 nan
70692655 82849 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2057456 82849 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
117772871 139258 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697621 139258 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
74223831 136231 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 2 6 2.1 Cc1c(-c2ccc(Oc3nccc4n[nH]cc34)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3671308 136231 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 2 6 2.1 Cc1c(-c2ccc(Oc3nccc4n[nH]cc34)cc2)n(C)c(=O)[nH]c1=O nan
15115518 15709 0 None -380 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109787 15709 0 None -380 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
135398737 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 7745 93 None -83 90 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
44447996 162282 0 None -44 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL404137 162282 0 None -44 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
145967572 171712 0 None -33 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 171712 0 None -33 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
122167 19013 13 None -56 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Dopamine receptor D1In vitro binding affinity towards Dopamine receptor D1
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
CHEMBL11845 19013 13 None -56 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Dopamine receptor D1In vitro binding affinity towards Dopamine receptor D1
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
44340302 16524 0 None -3 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 16524 0 None -3 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25139329 193882 0 None -11 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL491466 193882 0 None -11 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
71583848 94506 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 94506 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
137636460 162899 0 None -120 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 162899 0 None -120 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
122189387 130020 0 None -45 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613873 130020 0 None -45 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
44400594 140353 0 None -85 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL371165 140353 0 None -85 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
240 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
2769 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
44279790 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
660 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL1729 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL560739 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
DB00604 7731 43 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
4420454 63033 6 None -41 5 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None -41 5 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10454684 211584 0 None -5623 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7508 211584 0 None -5623 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44340186 16432 0 None -45 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 16432 0 None -45 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
137640152 163532 0 None -10715 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4070604 163532 0 None -10715 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
44437897 159832 0 None -776 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397592 159832 0 None -776 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
90644059 118807 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 118807 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
25132869 110072 0 None -269 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 110072 0 None -269 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
154705296 183173 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4444691 183173 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 183173 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
154726793 183012 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4590966 183012 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 183012 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
45481839 204873 0 None -22 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 4 1 2 3.7 CCCCC1NCCc2cc(Cl)c(OC)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574418 204873 0 None -22 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 4 1 2 3.7 CCCCC1NCCc2cc(Cl)c(OC)cc21 10.1016/j.bmc.2009.05.079
46227284 206494 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
CHEMBL593394 206494 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
11351639 67298 0 None -93 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 67298 0 None -93 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
44299993 108699 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL301003 108699 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
72708058 98970 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425368 98970 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
25256817 188205 0 None -169 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 445 6 0 3 5.0 O=C1c2ccccc2CCCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476394 188205 0 None -169 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 445 6 0 3 5.0 O=C1c2ccccc2CCCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
44582489 196579 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 3.9 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL516270 196579 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 3.9 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
14198596 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
145969667 171744 0 None -30 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 171744 0 None -30 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
14198596 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00118a012
CHEMBL299056 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00118a012
13678327 208833 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 329 8 3 4 4.1 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
CHEMBL60861 208833 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 329 8 3 4 4.1 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
11151583 136241 0 None -2 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 327 2 1 5 2.6 CN1CCN(C2=Cn3c(CO)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL367180 136241 0 None -2 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 327 2 1 5 2.6 CN1CCN(C2=Cn3c(CO)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
44415738 86669 0 None 22 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 1 1 4 6.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C(=O)Nc3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212384 86669 0 None 22 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 1 1 4 6.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C(=O)Nc3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
135995891 209739 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62996 209739 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
154726046 183090 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442408 183090 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595266 183090 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
44582678 188353 0 None -12 10 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 188353 0 None -12 10 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
15696482 86334 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2114209 86334 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
14198596 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 108420 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
14198600 108668 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 108668 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
14198601 107678 1 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL293828 107678 1 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
44582115 188454 0 None -154 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 6 0 3 4.6 O=C1c2ccccc2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477646 188454 0 None -154 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 6 0 3 4.6 O=C1c2ccccc2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
180 7189 56 None -109 40 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 7189 56 None -109 40 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 7189 56 None -109 40 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 7189 56 None -109 40 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 7189 56 None -109 40 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
130907 201462 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL53294 201462 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
1704 10295 85 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
4331799 10295 85 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
CHEMBL1334465 10295 85 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
23656545 153548 0 None -83 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 3 3.5 COc1cc2c3c(c1)-c1c(ccc(C)c1O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2007.05.057
CHEMBL392447 153548 0 None -83 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 3 3.5 COc1cc2c3c(c1)-c1c(ccc(C)c1O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2007.05.057
14198600 108668 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 108668 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
1212 8443 50 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
204 8443 50 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
3372 8443 50 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
CHEMBL726 8443 50 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
DB00623 8443 50 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
14198601 107678 1 None -1 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL293828 107678 1 None -1 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
13678309 201705 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 255 1 3 3 2.5 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2 10.1021/jm00160a018
CHEMBL54168 201705 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 255 1 3 3 2.5 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2 10.1021/jm00160a018
3036864 209533 19 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
10084583 111555 4 None -33 6 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 111555 4 None -33 6 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
5281878 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
5281881 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
948 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
968 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
CHEMBL42055 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
CHEMBL54661 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
DB00875 8441 35 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
44578927 196441 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 335 4 0 3 4.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CC)c1-3 10.1016/j.bmc.2008.08.056
CHEMBL515187 196441 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 335 4 0 3 4.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CC)c1-3 10.1016/j.bmc.2008.08.056
11976 7707 59 None -12 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
667467 7707 59 None -12 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
CHEMBL908 7707 59 None -12 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
DB01239 7707 59 None -12 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
10684714 107086 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 107086 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 107086 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
9796958 153356 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 153356 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 153356 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 153356 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10684715 167419 0 None 11 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL41132 167419 0 None 11 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
11089340 19660 0 None -5 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 2 0 4 4.0 CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118889 19660 0 None -5 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 2 0 4 4.0 CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
17756101 105360 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 105360 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
86764103 139215 13 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697578 139215 13 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
10457445 109970 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL308295 109970 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
10656804 123337 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL336366 123337 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
1621 9207 17 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 9207 17 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 9207 17 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 9207 17 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 9207 17 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
44276414 104404 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL27101 104404 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
45482169 204617 0 None -6 4 Pig 6.8 pKi = 6.8 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
CHEMBL572379 204617 0 None -6 4 Pig 6.8 pKi = 6.8 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
135398737 7745 93 None -44 90 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 7745 93 None -44 90 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 7745 93 None -44 90 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 7745 93 None -44 90 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 7745 93 None -44 90 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
44209472 76947 2 None -97 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 76947 2 None -97 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
90644228 118563 0 None -29 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 118563 0 None -29 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
11092112 214407 0 None -3162 9 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 214407 0 None -3162 9 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
44403232 77851 0 None -112 5 Pig 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL195247 77851 0 None -112 5 Pig 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
44436610 98724 0 None -234 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241436 98724 0 None -234 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
130907 201462 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL53294 201462 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
52937680 67947 0 None -3235 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
CHEMBL1765632 67947 0 None -3235 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
137659990 166009 0 None -3019 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 166009 0 None -3019 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
57393627 76082 0 None -199 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 76082 0 None -199 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
11077918 213373 0 None -13 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
CHEMBL88937 213373 0 None -13 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
46869265 23029 0 None -4 7 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 23029 0 None -4 7 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
73353534 97833 0 None -4168 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397477 97833 0 None -4168 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
71733932 97827 0 None -24547 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 97827 0 None -24547 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
23642427 98574 0 None -38904 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL241169 98574 0 None -38904 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
24824061 104673 0 None -25 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
CHEMBL272396 104673 0 None -25 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
10021692 153160 19 None -23442 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL392158 153160 19 None -23442 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
132060743 169015 0 None -7 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 169015 0 None -7 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
145969667 171744 0 None -30 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 171744 0 None -30 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
228 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
33 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
6005 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
CHEMBL53 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
DB00714 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
11559090 162340 0 None -60 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL404352 162340 0 None -60 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
44567689 190588 0 None -7 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 309 3 1 3 3.9 CCCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
CHEMBL480525 190588 0 None -7 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 309 3 1 3 3.9 CCCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
145979855 173307 0 None -83 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4279136 173307 0 None -83 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
72708058 98970 0 None 1 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425368 98970 0 None 1 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
70690497 82838 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057438 82838 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
70690497 82838 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL2057438 82838 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
681 8247 72 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
940 8247 72 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
947 8247 72 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
CHEMBL59 8247 72 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
DB00988 8247 72 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
13903144 106862 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
CHEMBL1743798 106862 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
CHEMBL287332 106862 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
46227317 206942 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 206942 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
45379377 14229 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
CHEMBL1086790 14229 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
10107367 109211 1 None -7 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 109211 1 None -7 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
11777127 32582 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 32582 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
117773975 139212 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 367 4 1 6 2.9 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1C nan
CHEMBL3697575 139212 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 367 4 1 6 2.9 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1C nan
4011 89183 49 None -64 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 89183 49 None -64 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
71722293 109252 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 109252 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 109252 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
135398737 7745 93 None -44 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 7745 93 None -44 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 7745 93 None -44 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 7745 93 None -44 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 7745 93 None -44 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
60165416 82071 0 None -478 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037431 82071 0 None -478 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
44439944 158648 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
CHEMBL396561 158648 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
49782600 24225 0 None -4 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257689 24225 0 None -4 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
127031397 145508 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 397 7 1 5 4.6 CCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3780140 145508 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 397 7 1 5 4.6 CCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
44401106 131105 0 None -29 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL363581 131105 0 None -29 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
9796255 135826 0 None -17 7 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL367045 135826 0 None -17 7 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
9796255 135826 0 None -17 7 Rat 7.7 pKi = 7.7 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm049629t
CHEMBL367045 135826 0 None -17 7 Rat 7.7 pKi = 7.7 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm049629t
10894826 17258 0 None -3 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL116542 17258 0 None -3 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
9884087 21409 0 None -4 2 Rat 7.7 pKi = 7.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.7 pKi = 7.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
71733935 97758 0 None -457 6 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2396663 97758 0 None -457 6 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
1242 10385 27 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
935 10385 27 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL286080 10385 27 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
25110707 19379 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186974 19379 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485036 19379 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
10594054 38187 1 None -562 4 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL140258 38187 1 None -562 4 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
14198600 108668 2 None 3 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 108668 2 None 3 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
54583898 68385 0 None -3801 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771114 68385 0 None -3801 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44412482 84934 0 None -4365 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210404 84934 0 None -4365 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
17475863 175563 3 None -660 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL437490 175563 3 None -660 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
53317208 65329 0 None -234 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 634 14 0 8 6.4 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCn2cc(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684029 65329 0 None -234 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 634 14 0 8 6.4 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCn2cc(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
24854106 167840 1 None -95 8 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
CHEMBL411663 167840 1 None -95 8 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
10960333 213763 0 None -2 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL91362 213763 0 None -2 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
44339953 116477 0 None -707 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 116477 0 None -707 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
21559988 120204 3 None -30 4 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318852 120204 3 None -30 4 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
9797495 75779 0 None -17378 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
CHEMBL1923292 75779 0 None -17378 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
44381279 65513 0 None -41 4 Bovine 4.7 pKi = 4.7 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168571 65513 0 None -41 4 Bovine 4.7 pKi = 4.7 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44415837 146317 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 3 1 5 5.9 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL379593 146317 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 3 1 5 5.9 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
154724369 183468 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4584372 183468 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598389 183468 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
681 8247 72 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
940 8247 72 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
947 8247 72 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
CHEMBL59 8247 72 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
DB00988 8247 72 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
6603800 10321 11 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
956 10321 11 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
CHEMBL63321 10321 11 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
5281148 210688 50 None 5 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 260 8 2 2 2.8 C=C[C@@H](O)C#CC#C[C@@H](O)/C=C\CCCCCCC 10.1016/j.bmc.2007.12.021
CHEMBL69018 210688 50 None 5 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 260 8 2 2 2.8 C=C[C@@H](O)C#CC#C[C@@H](O)/C=C\CCCCCCC 10.1016/j.bmc.2007.12.021
14198585 107578 1 None 1 4 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 107578 1 None 1 4 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
44582705 193775 0 None -12 13 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 193775 0 None -12 13 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
2351 10059 64 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
12488 8438 56 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 8438 56 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 8438 56 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 8438 56 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
10338282 41461 1 None -2 6 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143022 41461 1 None -2 6 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
13678325 108697 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 313 8 2 3 4.4 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
CHEMBL300995 108697 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 313 8 2 3 4.4 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
6937303 209986 7 None -43 4 Bovine 4.7 pKi = 4.7 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64376 209986 7 None -43 4 Bovine 4.7 pKi = 4.7 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
44278364 106196 0 None -169 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 334 6 0 2 3.9 O=C1c2ccccc2CN1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL282822 106196 0 None -169 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 334 6 0 2 3.9 O=C1c2ccccc2CN1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
68950 134317 12 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 8 0 2 4.0 CCN(CC)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL366265 134317 12 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 8 0 2 4.0 CCN(CC)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
191 7191 98 None -26 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 7191 98 None -26 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 7191 98 None -26 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 7191 98 None -26 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 7191 98 None -26 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
242 7258 124 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
34 7258 124 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
60795 7258 124 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
CHEMBL1112 7258 124 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
DB01238 7258 124 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
46931072 208824 1 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 208824 1 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
15711870 19728 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1189332 19728 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL538520 19728 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
164610779 191862 0 None -81 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 558 7 2 5 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(I)c(OC)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4855891 191862 0 None -81 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 558 7 2 5 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(I)c(OC)c1)CC2 10.1016/j.bmcl.2021.128047
10046389 68190 0 None -1122 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 68190 0 None -1122 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
15136 114887 2 None -154 2 Rat 5.7 pKi = 5.7 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL319557 114887 2 None -154 2 Rat 5.7 pKi = 5.7 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
44432812 94343 0 None -5 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 3 2 3 3.4 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL233567 94343 0 None -5 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 3 2 3 3.4 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
154703541 183078 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4541924 183078 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 183078 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
11186895 94282 25 None -5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
CHEMBL2334885 94282 25 None -5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
1353 8692 93 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
3559 8692 93 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
86 8692 93 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
CHEMBL54 8692 93 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
DB00502 8692 93 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
46231589 208080 0 None 999 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNc3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL604108 208080 0 None 999 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNc3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
37459 7533 13 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
62 7533 13 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
CHEMBL8514 7533 13 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
142405827 186644 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 421 2 1 4 6.1 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(OC(F)(F)F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4745489 186644 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 421 2 1 4 6.1 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(OC(F)(F)F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
142405818 187638 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 367 2 1 4 5.2 COc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4757297 187638 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 367 2 1 4 5.2 COc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
15937728 26767 0 None 288 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C(C2C=CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL130328 26767 0 None 288 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C(C2C=CCCC2)C1 10.1016/S0960-894X(00)80155-9
11623343 147620 1 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 147620 1 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
44415702 146677 0 None 87 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 2 1 5 5.4 Cc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL379942 146677 0 None 87 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 2 1 5 5.4 Cc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
16665071 100176 0 None -8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245764 100176 0 None -8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
10004036 102004 0 None 33 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL256075 102004 0 None 33 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
71563084 94346 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335736 94346 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
46231847 207353 0 None 3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 207353 0 None 3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
6603950 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64875 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
6603950 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL64875 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
16090814 88356 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL216258 88356 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
6603950 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64875 210103 9 None -6 8 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10935201 27656 0 None 758 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.1 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL131054 27656 0 None 758 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.1 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCCC2)C1 10.1016/S0960-894X(00)80155-9
16090814 88356 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 88356 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
134151764 159923 0 None 31 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 433 4 2 5 4.3 CCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3976659 159923 0 None 31 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 433 4 2 5 4.3 CCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
1238 209953 24 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64249 209953 24 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
15115523 115646 1 None 691 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 346 1 2 3 3.4 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N)cc2)C1 10.1021/jm00115a012
CHEMBL321042 115646 1 None 691 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 346 1 2 3 3.4 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N)cc2)C1 10.1021/jm00115a012
11315462 207245 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)C4CC4)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL598516 207245 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)C4CC4)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
46231833 207690 0 None 218 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 384 2 2 3 4.3 CCC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL601634 207690 0 None 218 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 384 2 2 3 4.3 CCC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
142405825 186618 0 None -24 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4745124 186618 0 None -24 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
134135947 151167 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 5 2 5 4.7 CCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3905947 151167 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 5 2 5 4.7 CCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
37459 7533 13 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
62 7533 13 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
CHEMBL8514 7533 13 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
46231782 207282 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 207282 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
46232064 208127 0 None 707 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 473 2 1 3 6.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(OC(F)(F)F)c4)c3CC[C@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604383 208127 0 None 707 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 473 2 1 3 6.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(OC(F)(F)F)c4)c3CC[C@H]21 10.1016/j.bmcl.2009.12.094
1238 209953 24 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64249 209953 24 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10662054 91187 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114444 91187 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219803 91187 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
146266 107474 8 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL292418 107474 8 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL540857 107474 8 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
46231772 208088 0 None 371 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL604132 208088 0 None 371 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
162676091 190103 0 None 512 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 401 2 1 4 5.7 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(OC(F)(F)F)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4797375 190103 0 None 512 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 401 2 1 4 5.7 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(OC(F)(F)F)ccc1N2 10.1016/j.bmcl.2020.127563
75202022 177589 2 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 177589 2 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
10537185 32457 0 None -12 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135224 32457 0 None -12 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
44415672 86949 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 86949 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
70690500 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.12.016
CHEMBL2057455 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.12.016
70690500 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
70690500 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 82848 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
44415689 145887 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 145887 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
46231846 208118 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 208118 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
17755867 92884 1 None -1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL231070 92884 1 None -1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
9993922 66740 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 282 1 0 2 3.5 CN1CCc2cccc3c2C(C1)CN3c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL173315 66740 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 282 1 0 2 3.5 CN1CCc2cccc3c2C(C1)CN3c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
46231768 206259 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL591685 206259 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11439190 208084 0 None 31 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 208084 0 None 31 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
37461 23906 14 None -3 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/j.bmcl.2021.128047
CHEMBL1255588 23906 14 None -3 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/j.bmcl.2021.128047
44268688 173354 0 None 37 2 Rat 8.5 pKi = 8.5 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
CHEMBL427996 173354 0 None 37 2 Rat 8.5 pKi = 8.5 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
4350931 176092 44 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
CHEMBL441618 176092 44 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
4350931 176092 44 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
CHEMBL441618 176092 44 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
1353 8692 93 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
3559 8692 93 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
86 8692 93 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
CHEMBL54 8692 93 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
DB00502 8692 93 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
44331310 114143 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9800292
CHEMBL317741 114143 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9800292
44415649 145202 0 None 162 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL377420 145202 0 None 162 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
135398745 9688 112 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
47 9688 112 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
CHEMBL715 9688 112 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
DB00334 9688 112 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
10894826 17258 0 None -3 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL116542 17258 0 None -3 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
10519435 178248 0 None 87 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL446350 178248 0 None 87 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10015045 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
CHEMBL119455 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
10015045 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960188q
CHEMBL119455 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960188q
10015045 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
CHEMBL119455 20424 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
16103 211417 47 None -2 4 Rat 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL73538 211417 47 None -2 4 Rat 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
155515982 176789 0 None -794 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None -794 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
56833464 75171 0 None -99 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916720 75171 0 None -99 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
14378574 115364 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL320397 115364 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
57390116 76073 0 None -323 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 76073 0 None -323 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
118709175 120200 0 None -107 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318848 120200 0 None -107 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10378194 204544 0 None -338 6 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 204544 0 None -338 6 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
10862425 123411 0 None -467 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
CHEMBL336930 123411 0 None -467 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
10613676 20628 0 None -165 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1021/jm060959i
CHEMBL119593 20628 0 None -165 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1021/jm060959i
10092819 23545 0 None -1412 11 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL124444 23545 0 None -1412 11 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
52947756 23942 0 None -478 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256170 23942 0 None -478 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
44319368 112841 0 None -7 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 112841 0 None -7 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
44319369 212598 0 None -11 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 212598 0 None -11 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
44380802 168470 0 None -131 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL413343 168470 0 None -131 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
6469693 86730 17 None -7079 6 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 86730 17 None -7079 6 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
44319369 212598 0 None -11 4 Bovine 4.7 pKi = 4.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 212598 0 None -11 4 Bovine 4.7 pKi = 4.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
2247 7293 81 None -61 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -61 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -61 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -61 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -61 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
24949857 188546 0 None -7413 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
CHEMBL477765 188546 0 None -7413 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
53318500 65324 0 None -57 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 630 10 0 7 6.9 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684024 65324 0 None -57 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 630 10 0 7 6.9 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
2993172 133945 4 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 133945 4 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
134551 7146 27 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
2105 9828 37 None -123 32 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
47811 9828 37 None -123 32 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
48 9828 37 None -123 32 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
CHEMBL531 9828 37 None -123 32 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
DB01186 9828 37 None -123 32 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
25212275 181200 0 None -4897 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL455288 181200 0 None -4897 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
25212276 196845 0 None -575 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517244 196845 0 None -575 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
135446209 16357 58 None -22 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
CHEMBL1125 16357 58 None -22 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
71061709 156306 0 None -14 12 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 156306 0 None -14 12 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
44582113 188414 0 None -169 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 364 6 0 4 2.7 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477434 188414 0 None -169 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 364 6 0 4 2.7 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
10474964 137249 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 137249 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 137249 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
5353853 24758 47 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
127262 20252 12 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL1193274 20252 12 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
46227325 206906 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
CHEMBL596179 206906 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
71474079 150042 0 None - 1 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3896731 150042 0 None - 1 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
10550785 170211 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 433 4 1 2 5.9 Oc1cc2c(cc1Br)CCN(C/C=C/c1ccccc1)CC2c1ccccc1 10.1021/jm960143p
CHEMBL419759 170211 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 433 4 1 2 5.9 Oc1cc2c(cc1Br)CCN(C/C=C/c1ccccc1)CC2c1ccccc1 10.1021/jm960143p
53359025 69127 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 69127 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
6603703 6996 10 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
9637 6996 10 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
CHEMBL291143 6996 10 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
2389 10104 118 None -489 66 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 10104 118 None -489 66 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 10104 118 None -489 66 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 10104 118 None -489 66 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 10104 118 None -489 66 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
13372 10531 30 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
86764100 10531 30 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
CHEMBL3697617 10531 30 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
DB14899 10531 30 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
6603820 102549 19 None -2 12 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 102549 19 None -2 12 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
135398737 7745 93 None -44 90 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
38 7745 93 None -44 90 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
722 7745 93 None -44 90 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
CHEMBL42 7745 93 None -44 90 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
DB00363 7745 93 None -44 90 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
75201901 173204 19 None -1 24 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None -1 24 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
17756101 105360 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL276778 105360 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
10903748 85251 0 None -10 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL2111781 85251 0 None -10 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
2435 10362 83 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 10362 83 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 10362 83 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 10362 83 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 10362 83 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
228 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
33 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
6005 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
CHEMBL53 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
DB00714 7233 28 None -30 23 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
53364153 70615 0 None -38 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803023 70615 0 None -38 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
135398737 7745 93 None -83 90 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
38 7745 93 None -83 90 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
722 7745 93 None -83 90 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
CHEMBL42 7745 93 None -83 90 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
DB00363 7745 93 None -83 90 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
52945819 24325 0 None -14 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258037 24325 0 None -14 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
127047996 146424 0 None -46 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 146424 0 None -46 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
137636351 162652 0 None -602 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 162652 0 None -602 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
25072002 162893 0 None -1047 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 162893 0 None -1047 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
122189388 130021 0 None -40 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 130021 0 None -40 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
44300865 208774 0 None -173 7 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 208774 0 None -173 7 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
44340302 16524 0 None -3 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 16524 0 None -3 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340376 117423 0 None -24 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 117423 0 None -24 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
54581963 68375 0 None -7762 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771105 68375 0 None -7762 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44300865 208774 0 None -173 7 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL60815 208774 0 None -173 7 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
9980998 37808 0 None -1819 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 37808 0 None -1819 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 37808 0 None -1819 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
45273442 203230 0 None -100 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL563078 203230 0 None -100 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44567594 179412 0 None -34 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL449461 179412 0 None -34 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
49783040 24462 0 None -446 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
CHEMBL1258494 24462 0 None -446 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
137660837 165859 0 None -3019 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 165859 0 None -3019 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
11154555 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL3085826 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 7587 62 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
15723715 20186 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1192815 20186 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL544118 20186 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
44316315 212298 0 None -1318 5 Bovine 4.7 pKi = 4.7 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL80845 212298 0 None -1318 5 Bovine 4.7 pKi = 4.7 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
44264622 103918 4 None -72 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL267853 103918 4 None -72 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44412268 85142 9 None -2089 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL211026 85142 9 None -2089 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
72544789 99907 0 None -912 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 99907 0 None -912 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
45379515 14228 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3[nH]c4ccccc4c3C21 10.1021/jm901291r
CHEMBL1086789 14228 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3[nH]c4ccccc4c3C21 10.1021/jm901291r
44448027 161809 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 481 4 0 5 4.1 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401567 161809 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 481 4 0 5 4.1 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
12301195 206495 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.2 COc1ccc2c(c1)CCN1CCc3ccccc3C21 10.1016/j.bmc.2009.08.028
CHEMBL593395 206495 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.2 COc1ccc2c(c1)CCN1CCc3ccccc3C21 10.1016/j.bmc.2009.08.028
9817779 121210 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL333246 121210 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
10085633 126774 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 290 4 1 3 2.4 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCOCC1)CC2 10.1016/0960-894X(95)00076-6
CHEMBL349997 126774 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 290 4 1 3 2.4 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCOCC1)CC2 10.1016/0960-894X(95)00076-6
15654855 109440 0 None 4 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3cc(Cl)ccc32)CC1 10.1021/jm00067a009
CHEMBL304493 109440 0 None 4 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3cc(Cl)ccc32)CC1 10.1021/jm00067a009
2337 10030 77 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 10030 77 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 10030 77 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 10030 77 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 10030 77 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
9927411 209832 0 None -89 4 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL63576 209832 0 None -89 4 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL4566600 220793 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
CHEMBL4745071 220793 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5212743
112500026 139240 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697602 139240 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)ncc(=O)n1C nan
118711262 120734 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1cccc(-c2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
CHEMBL3325913 120734 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1cccc(-c2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
9817779 121210 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL333246 121210 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
168290235 199747 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
9998826 127255 0 None -33113 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 127255 0 None -33113 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
2389 10104 118 None -346 66 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
5073 10104 118 None -346 66 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
96 10104 118 None -346 66 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
CHEMBL85 10104 118 None -346 66 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
DB00734 10104 118 None -346 66 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
9884087 21409 0 None -4 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
44415624 86880 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213193 86880 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415577 86920 0 None 20 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 436 2 1 7 3.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccon3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213372 86920 0 None 20 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 436 2 1 7 3.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccon3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
25142456 89181 2 None -10 9 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None -10 9 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
439654 23270 39 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL1235966 23270 39 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
21527771 76931 1 None -8 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 76931 1 None -8 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
10903748 85251 0 None -10 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL2111781 85251 0 None -10 2 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10830234 107153 0 None 20 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289867 107153 0 None 20 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
11186523 134289 0 None -15 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL366164 134289 0 None -15 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
44408818 146943 1 None -12 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL380330 146943 1 None -12 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
53361301 70616 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1803024 70616 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
54585810 68378 0 None -22 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771108 68378 0 None -22 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
53361301 70616 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803024 70616 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53364226 70620 0 None -67 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803028 70620 0 None -67 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
118709160 120183 0 None -18 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318832 120183 0 None -18 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709161 120184 0 None -83 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318833 120184 0 None -83 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10524751 64128 0 None -1 4 Bovine 5.7 pKi = 5.7 Binding
Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL165171 64128 0 None -1 4 Bovine 5.7 pKi = 5.7 Binding
Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
11036641 38552 0 None -147 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL140612 38552 0 None -147 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
11517928 83878 0 None -18 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL207543 83878 0 None -18 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
15548770 73224 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1802234 73224 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852041 73224 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
122181333 128652 0 None -1548 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 128652 0 None -1548 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
57402365 76070 0 None -169 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 76070 0 None -169 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
44270558 172067 0 None -812 4 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL423247 172067 0 None -812 4 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44400553 77554 0 None -2398 5 Pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 77554 0 None -2398 5 Pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
15467372 175889 0 None -138 4 Bovine 4.7 pKi = 4.7 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL440120 175889 0 None -138 4 Bovine 4.7 pKi = 4.7 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
44264644 211522 0 None -1737 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7442 211522 0 None -1737 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
45269161 203114 0 None -181 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL562384 203114 0 None -181 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
46850462 83337 0 None -16 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccccc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
CHEMBL2062849 83337 0 None -16 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccccc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
46850464 83339 0 None -87 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062851 83339 0 None -87 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
5353432 104271 89 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 104271 89 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
45481889 205794 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 637 10 2 10 5.4 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5nsc6ccccc56)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
CHEMBL585741 205794 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 637 10 2 10 5.4 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5nsc6ccccc56)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
90644062 118811 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 118811 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
90644062 118811 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 118811 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44448065 162259 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL404037 162259 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
117773891 139203 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 379 5 1 6 3.1 Cc1cc(Oc2ncccc2OC2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697566 139203 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 379 5 1 6 3.1 Cc1cc(Oc2ncccc2OC2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
145979741 173464 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4282096 173464 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
46231835 207611 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 410 2 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCCCC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL600998 207611 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 410 2 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCCCC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL1200633 215379 3 None -7 8 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
112500027 139241 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697603 139241 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
44320257 212954 0 None -5 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86325 212954 0 None -5 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
49783209 24381 0 None -3981 26 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat dopamine D1 receptorBinding affinity to rat dopamine D1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -3981 26 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat dopamine D1 receptorBinding affinity to rat dopamine D1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
19795148 123368 0 None 97 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 265 0 1 2 3.3 CN1CCc2cc(Cl)c(O)cc2C2(CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL336610 123368 0 None 97 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 265 0 1 2 3.3 CN1CCc2cc(Cl)c(O)cc2C2(CCCC2)C1 10.1016/S0960-894X(00)80155-9
44447998 162172 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 363 6 0 3 5.3 CCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL403550 162172 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 363 6 0 3 5.3 CCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415844 86901 0 None 20 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3nccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213278 86901 0 None 20 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3nccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
17756102 92919 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 92919 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
15069442 107477 0 None 104 2 Rat 7.6 pKi = 7.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL292451 107477 0 None 104 2 Rat 7.6 pKi = 7.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
71110293 150157 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 150157 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
71110293 150157 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 150157 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
70682088 82843 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 82843 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
117773010 139231 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.9 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C nan
CHEMBL3697593 139231 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.9 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C nan
10947658 35475 0 None -208 16 Mouse 6.6 pKi = 6.6 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 35475 0 None -208 16 Mouse 6.6 pKi = 6.6 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
6603954 209384 2 None -81 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL612083 209384 2 None -81 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
11392229 69753 0 None -15 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 293 1 0 3 2.9 Cc1ccc2n1Cc1ccccc1C=C2N1CCN(C)CC1 10.1021/jm049629t
CHEMBL178564 69753 0 None -15 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 293 1 0 3 2.9 Cc1ccc2n1Cc1ccccc1C=C2N1CCN(C)CC1 10.1021/jm049629t
44360984 41855 0 None -208 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
CHEMBL143352 41855 0 None -208 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
11516033 145896 5 None -1949 6 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL378680 145896 5 None -1949 6 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
54583897 68376 0 None -1445 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771106 68376 0 None -1445 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363109 70622 0 None -691 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803030 70622 0 None -691 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
137660046 166122 0 None -3235 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 166122 0 None -3235 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
52937871 67946 0 None -588 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
CHEMBL1765631 67946 0 None -588 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
122177644 127990 0 None -19054 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 127990 0 None -19054 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
56926585 75780 0 None -5495 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923293 75780 0 None -5495 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44381424 65845 0 None -190 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169562 65845 0 None -190 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
44381432 127496 0 None -6 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL354748 127496 0 None -6 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
72301 192897 76 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL487182 192897 76 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
44591134 182979 0 None -194 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459373 182979 0 None -194 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
154726381 183306 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 183306 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 183306 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
90644057 118809 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 118809 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
90644057 118809 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 118809 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
145992269 173732 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
CHEMBL4287192 173732 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
46227273 206590 0 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
CHEMBL594127 206590 0 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
135398737 7745 93 None -83 90 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 7745 93 None -83 90 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 7745 93 None -83 90 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 7745 93 None -83 90 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 7745 93 None -83 90 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
14198576 204667 0 None -2 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 3 1 2 3.8 COc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL572720 204667 0 None -2 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 3 1 2 3.8 COc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
228 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
33 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
6005 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
CHEMBL53 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
DB00714 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
228 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
33 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
6005 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
CHEMBL53 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
DB00714 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
228 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
33 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
6005 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
CHEMBL53 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
DB00714 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
228 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
33 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
6005 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
CHEMBL53 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
DB00714 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
44415613 84842 0 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 543 3 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCN(C)CC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL210016 84842 0 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 543 3 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCN(C)CC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
72708061 98974 0 None -1 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425372 98974 0 None -1 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL5274285 200585 0 None -20 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in HEK293 cell membrane assessed as inhibition constantDisplacement of [3H]SCH23390 from D1 receptor in HEK293 cell membrane assessed as inhibition constant
ChEMBL 415 4 1 2 5.3 Fc1ccc(CN2CCCC23CCN(Cc2cc4ccc(Cl)cc4[nH]2)C3)cc1F 10.1016/j.ejmech.2022.114840
44415645 146122 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 613 4 1 7 6.5 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc4c(c3)OCCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL379286 146122 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 613 4 1 7 6.5 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc4c(c3)OCCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44209480 76945 0 None -218 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 76945 0 None -218 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
10264172 17205 0 None -7413 2 Rat 4.6 pKi = 4.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 2 2 3.1 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960188q
CHEMBL116367 17205 0 None -7413 2 Rat 4.6 pKi = 4.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 2 2 3.1 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960188q
3037308 50853 27 None -99 6 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 50853 27 None -99 6 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
9928073 210428 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL67284 210428 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00030a011
10108504 45680 0 None 6 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3ccccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL146741 45680 0 None 6 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3ccccc3Oc3ncccc32)CC1 10.1021/jm00030a011
44582518 188372 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.6 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477055 188372 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.6 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
3036864 209533 19 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
44385451 66366 0 None -7 2 Rat 7.6 pKi = 7.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 284 3 0 2 3.9 Cc1cccc2c1C(CN(C)C)CN2c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL171903 66366 0 None -7 2 Rat 7.6 pKi = 7.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 284 3 0 2 3.9 Cc1cccc2c1C(CN(C)C)CN2c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
13838745 101507 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
CHEMBL25305 101507 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
1353 8692 93 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
3559 8692 93 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
86 8692 93 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
CHEMBL54 8692 93 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
DB00502 8692 93 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
15937721 25877 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 255 2 1 3 2.6 CCOC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL128917 25877 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 255 2 1 3 2.6 CCOC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
44415670 145694 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 565 2 1 5 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL378341 145694 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 565 2 1 5 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415745 173101 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL427230 173101 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
86764211 139224 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697587 139224 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90140334 136191 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc2n[nH]cc2c(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)n1 nan
CHEMBL3671270 136191 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc2n[nH]cc2c(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)n1 nan
44276535 105165 0 None 50 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL275379 105165 0 None 50 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
10432808 65523 0 None -6 4 Bovine 6.6 pKi = 6.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168611 65523 0 None -6 4 Bovine 6.6 pKi = 6.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
2389 10104 118 None -489 66 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 10104 118 None -489 66 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 10104 118 None -489 66 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 10104 118 None -489 66 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 10104 118 None -489 66 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10042942 162281 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1OC)-c1c(OC)c(O)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL404136 162281 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1OC)-c1c(OC)c(O)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
137642380 165286 0 None -48 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 165286 0 None -48 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
90644227 118557 0 None -186 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 118557 0 None -186 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
228 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
33 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
6005 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
CHEMBL53 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
DB00714 7233 28 None -30 23 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
9928073 210428 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL67284 210428 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00067a009
53362716 70736 0 None -26 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
CHEMBL1806871 70736 0 None -26 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
49783039 24425 0 None -954 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
CHEMBL1258383 24425 0 None -954 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
57400557 76087 0 None -1995 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 76087 0 None -1995 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
15654854 109032 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cccnc3Nc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL303173 109032 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cccnc3Nc3ccccc32)CC1 10.1021/jm00067a009
11589069 103022 0 None -1479 8 Human 5.6 pKi = 5.6 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 103022 0 None -1479 8 Human 5.6 pKi = 5.6 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
15115513 115457 0 None -218 2 Human 4.6 pKi = 4.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL320779 115457 0 None -218 2 Human 4.6 pKi = 4.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
681 8247 72 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
940 8247 72 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
947 8247 72 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
CHEMBL59 8247 72 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
DB00988 8247 72 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
44299917 176228 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@@H]21 10.1021/jm00128a038
CHEMBL442740 176228 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@@H]21 10.1021/jm00128a038
90134304 173293 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
CHEMBL4278861 173293 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
71562963 94351 0 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335741 94351 0 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
10691657 126692 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 387 3 0 3 5.1 CCCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL349311 126692 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 387 3 0 3 5.1 CCCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
168294767 199798 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
117773347 139205 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 378 4 1 6 2.8 Cc1cc(Oc2ncccc2N2CCC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697568 139205 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 378 4 1 6 2.8 Cc1cc(Oc2ncccc2N2CCC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
71110290 153938 0 None - 1 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3927835 153938 0 None - 1 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
15711860 20630 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1195937 20630 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL555619 20630 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
14198588 178286 2 None 2 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL446396 178286 2 None 2 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
44320001 212795 0 None 2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 212795 0 None 2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44591135 196956 0 None -158 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517407 196956 0 None -158 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
71110293 150157 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 150157 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
135398745 9688 112 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
47 9688 112 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
CHEMBL715 9688 112 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
DB00334 9688 112 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
1353 8692 93 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 8692 93 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 8692 93 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 8692 93 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 8692 93 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
1242 10385 27 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
935 10385 27 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
CHEMBL286080 10385 27 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
75306277 116031 0 None -12 23 Human 7.6 pKi = 7.6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 116031 0 None -12 23 Human 7.6 pKi = 7.6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
9884087 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
71474026 161078 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
CHEMBL3986624 161078 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
11718008 82066 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 82066 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
44415954 87876 0 None 72 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 467 6 1 5 5.4 CCCC(CCC)C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL215581 87876 0 None 72 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 467 6 1 5 5.4 CCCC(CCC)C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
135398745 9688 112 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 9688 112 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 9688 112 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 9688 112 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
53364154 70617 0 None -13 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803025 70617 0 None -13 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
45273443 202410 0 None -66 4 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL556288 202410 0 None -66 4 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
137644966 165273 0 None -363 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 165273 0 None -363 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
122191607 130500 0 None -346 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 130500 0 None -346 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
56837636 76072 0 None -177 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 76072 0 None -177 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
44401042 131607 0 None -67 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL364270 131607 0 None -67 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
11575799 84904 0 None -2511 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL210341 84904 0 None -2511 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
25256814 188391 0 None -1318 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 188391 0 None -1318 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363110 70625 0 None -194 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803050 70625 0 None -194 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
24823922 167572 0 None -15 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
CHEMBL411437 167572 0 None -15 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
11725531 60828 2 None -1659 5 Bovine 5.6 pKi = 5.6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 60828 2 None -1659 5 Bovine 5.6 pKi = 5.6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
15522515 104937 0 None -1479 4 Bovine 4.6 pKi = 4.6 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL273860 104937 0 None -1479 4 Bovine 4.6 pKi = 4.6 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
71734028 97828 0 None -7762 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397390 97828 0 None -7762 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
2389 10104 118 None -346 66 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 10104 118 None -346 66 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 10104 118 None -346 66 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 10104 118 None -346 66 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 10104 118 None -346 66 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
44320002 113818 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315535 113818 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44582491 188334 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 6 0 4 3.3 COc1ccccc1N1CCN(CCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476641 188334 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 6 0 4 3.3 COc1ccccc1N1CCN(CCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
10022123 60090 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL159969 60090 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL92673 60090 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
71562966 94348 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
CHEMBL2335738 94348 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
44478261 199076 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 0 3 6 3.0 CN1CCc2c3c(cc4nc(N)sc24)-c2c(ccc(O)c2O)C[C@H]31 10.1016/j.bmc.2008.05.077
CHEMBL520610 199076 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 0 3 6 3.0 CN1CCc2c3c(cc4nc(N)sc24)-c2c(ccc(O)c2O)C[C@H]31 10.1016/j.bmc.2008.05.077
175 10427 44 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
68186 10427 44 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
CHEMBL79834 10427 44 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
145988779 174058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
CHEMBL4293356 174058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
72164182 98925 0 None -41 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 98925 0 None -41 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
10092819 23545 0 None -2454 11 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
CHEMBL124444 23545 0 None -2454 11 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
44415647 146018 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 639 5 1 6 7.6 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL378893 146018 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 639 5 1 6 7.6 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
164612037 192156 0 None -144 20 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -144 20 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
57396484 76944 2 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940417 76944 2 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
13015797 212676 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
CHEMBL83915 212676 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
44415836 86911 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 4 1 5 5.9 CCCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213335 86911 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 4 1 5 5.9 CCCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
70607606 183983 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635277 183983 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
6852376 98374 13 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL1467585 98374 13 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL24077 98374 13 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL503958 98374 13 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
72699812 121964 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 315 2 1 4 3.7 CCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344456 121964 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 315 2 1 4 3.7 CCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
10566865 122757 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL335515 122757 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
10015045 20424 1 None -2 6 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL119455 20424 1 None -2 6 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
86764215 139235 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697597 139235 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
14198587 209910 1 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm00129a006
CHEMBL64117 209910 1 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm00129a006
11728201 20751 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL119687 20751 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL120512 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
15115514 15843 0 None -54 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109897 15843 0 None -54 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
90644061 118810 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 118810 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
136056636 118565 0 None -309 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 118565 0 None -309 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709174 120199 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318847 120199 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10917953 214767 0 None -7585 10 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 214767 0 None -7585 10 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
71583849 94507 0 None -147 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336893 94507 0 None -147 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
14659268 86413 2 None -35 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL2115032 86413 2 None -35 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
122180956 128549 0 None -263 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 128549 0 None -263 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
122177641 127987 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 127987 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
72544566 99906 0 None -1318 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 99906 0 None -1318 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
9865384 180274 35 None -30902 7 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL45305 180274 35 None -30902 7 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
10014924 114048 0 None -1548 5 Bovine 4.6 pKi = 4.6 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL316983 114048 0 None -1548 5 Bovine 4.6 pKi = 4.6 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
11472028 73541 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 1 3 3.2 OC(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
CHEMBL185875 73541 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 1 3 3.2 OC(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
15711855 20184 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192799 20184 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL544099 20184 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
11696813 194697 12 None -316 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm100294b
CHEMBL496739 194697 12 None -316 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm100294b
90644061 118810 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 118810 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
72708126 98977 0 None -7 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425375 98977 0 None -7 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
14198588 178286 2 None 2 2 Rat 4.6 pKi = 4.6 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 178286 2 None 2 2 Rat 4.6 pKi = 4.6 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
57401706 76946 0 None -45 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 76946 0 None -45 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44320218 213203 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
CHEMBL87897 213203 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
10993765 85542 0 None -10 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 433 5 0 5 4.1 COc1ccccc1N1CCN(CC2CCN(C(=O)c3cc4ccccc4o3)CC2)CC1 10.1021/jm0211220
CHEMBL2112643 85542 0 None -10 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 433 5 0 5 4.1 COc1ccccc1N1CCN(CC2CCN(C(=O)c3cc4ccccc4o3)CC2)CC1 10.1021/jm0211220
91899757 136218 0 None - 1 Human 6.6 pKi = 6.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-n1c(C)nc2cnccc21 nan
CHEMBL3671296 136218 0 None - 1 Human 6.6 pKi = 6.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-n1c(C)nc2cnccc21 nan
1971 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
25256816 188387 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477206 188387 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
9884087 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
21533446 76930 0 None -7 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 76930 0 None -7 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
11728201 20751 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL119687 20751 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL120512 21409 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
70684965 84609 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL2092940 84609 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
1353 8692 93 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 8692 93 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 8692 93 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 8692 93 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 8692 93 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
44249745 202222 1 None -363 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL552373 202222 1 None -363 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL567286 202222 1 None -363 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
24878061 148189 0 None 25 2 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 148189 0 None 25 2 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
10061323 18678 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL118254 18678 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
53364227 70621 0 None -50 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803029 70621 0 None -50 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
10061323 18678 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL118254 18678 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
11405107 205842 0 None -32 4 Bovine 5.6 pKi = 5.6 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
CHEMBL58662 205842 0 None -32 4 Bovine 5.6 pKi = 5.6 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
44403210 77318 0 None -630 5 Pig 5.6 pKi = 5.6 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194727 77318 0 None -630 5 Pig 5.6 pKi = 5.6 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
9970201 177422 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
CHEMBL445129 177422 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
52938728 65328 0 None -1000 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684028 65328 0 None -1000 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
137636066 163012 0 None -1698 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 163012 0 None -1698 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
4150 7575 39 None -69 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
5288 7575 39 None -69 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
644019 7575 39 None -69 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
CHEMBL190461 7575 39 None -69 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
DB09061 7575 39 None -69 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
11689612 86614 0 None -28840 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
CHEMBL212160 86614 0 None -28840 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
44412269 84875 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210232 84875 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
44412269 84875 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL210232 84875 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
45271653 202014 0 None -2238 4 Bovine 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL550920 202014 0 None -2238 4 Bovine 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
10046389 68190 0 None -1122 5 Bovine 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 68190 0 None -1122 5 Bovine 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
135 9310 43 None -91 56 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 9310 43 None -91 56 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 9310 43 None -91 56 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 9310 43 None -91 56 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 9310 43 None -91 56 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
44406077 139596 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
CHEMBL370136 139596 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
90644071 118819 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 118819 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
131396 213514 6 None -549 5 Rat 5.6 pKi = 5.6 Binding
Compound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligandCompound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligand
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm00092a024
CHEMBL89934 213514 6 None -549 5 Rat 5.6 pKi = 5.6 Binding
Compound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligandCompound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligand
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm00092a024
118711255 120730 0 None -26 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(NCc3cccc(Cl)c3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325905 120730 0 None -26 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(NCc3cccc(Cl)c3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
45269964 20393 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194295 20393 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550180 20393 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
10825256 16950 0 None -6 3 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 260 0 0 2 3.3 CN1CCc2cccc3c2[C@H]1Cc1cccc(C#N)c1-3 10.1021/jm960189i
CHEMBL115969 16950 0 None -6 3 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 260 0 0 2 3.3 CN1CCc2cccc3c2[C@H]1Cc1cccc(C#N)c1-3 10.1021/jm960189i
44432811 94342 0 None -5 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 323 3 1 3 4.2 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL233566 94342 0 None -5 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 323 3 1 3 4.2 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1016/j.bmcl.2007.05.057
44366021 127805 0 None - 1 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
CHEMBL356597 127805 0 None - 1 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
44415559 86938 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213444 86938 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415673 146022 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 545 4 1 7 6.1 CCOc1c(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)sc2ccccc12 10.1016/j.bmcl.2006.06.022
CHEMBL378914 146022 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 545 4 1 7 6.1 CCOc1c(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)sc2ccccc12 10.1016/j.bmcl.2006.06.022
16104 168696 19 None -1 5 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL415300 168696 19 None -1 5 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
74223830 136228 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671305 136228 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
16104 168696 19 None -1 5 Rat 7.6 pKi = 7.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL415300 168696 19 None -1 5 Rat 7.6 pKi = 7.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
17755999 149663 1 None -5 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL389357 149663 1 None -5 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
86767095 136205 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 345 3 1 5 4.1 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671284 136205 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 345 3 1 5 4.1 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
10566865 122757 0 None -4 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL335515 122757 0 None -4 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
44408818 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
44408818 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
CHEMBL380330 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
44408818 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 146943 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
45379370 14295 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 14295 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
10090424 41471 1 None -3 6 Rat 7.5 pKi = 7.5 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143027 41471 1 None -3 6 Rat 7.5 pKi = 7.5 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
70692656 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2057457 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.12.016
70692656 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057457 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692656 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
70692656 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 82850 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
44276651 106516 0 None 32 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL284959 106516 0 None 32 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
15225749 87460 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 341 0 1 5 3.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(N)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL215140 87460 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 341 0 1 5 3.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(N)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
137651073 164247 0 None -53 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 164247 0 None -53 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
118709162 120185 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318834 120185 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10689581 106939 0 None 1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL287931 106939 0 None 1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
44380770 172491 0 None -91 4 Bovine 5.6 pKi = 5.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL424575 172491 0 None -91 4 Bovine 5.6 pKi = 5.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
11706497 84952 0 None -776 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 84952 0 None -776 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
56833379 75109 0 None -234 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1916550 75109 0 None -234 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
44340415 15350 0 None -3 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 15350 0 None -3 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
127045854 146342 0 None -218 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 146342 0 None -218 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127046949 146687 0 None -446 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 146687 0 None -446 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
24936042 164368 0 None -218 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 164368 0 None -218 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
57390115 76071 0 None -575 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 76071 0 None -575 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
24824065 104727 0 None -1 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
CHEMBL272602 104727 0 None -1 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
10404144 212081 23 None -2187 10 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL7927 212081 23 None -2187 10 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
14198593 205453 1 None 4 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 205453 1 None 4 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
14198594 206882 1 None 6 2 Human 6.6 pKi = 6.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNC[C@H]2c1ccccc1 10.1021/jm00129a006
CHEMBL59603 206882 1 None 6 2 Human 6.6 pKi = 6.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNC[C@H]2c1ccccc1 10.1021/jm00129a006
44582178 188038 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 378 6 0 4 3.1 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476185 188038 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 378 6 0 4 3.1 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
9951008 213176 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87717 213176 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm981094e
9951008 213176 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87717 213176 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm00042a009
3561 25849 39 None -1 11 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 25849 39 None -1 11 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
15711852 20111 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192193 20111 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL543389 20111 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
5041 10067 6 None -11220 6 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
981 10067 6 None -11220 6 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
CHEMBL4096543 10067 6 None -11220 6 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
15711851 20312 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL1193797 20312 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL545264 20312 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
14198586 208612 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 208612 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
91899758 136219 0 None - 1 Human 6.5 pKi = 6.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cc(=O)[nH]nc1C nan
CHEMBL3671297 136219 0 None - 1 Human 6.5 pKi = 6.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cc(=O)[nH]nc1C nan
117773787 139219 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.7 Cc1cc(Oc2ncccc2C2COC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697582 139219 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.7 Cc1cc(Oc2ncccc2C2COC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
10333195 54960 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
CHEMBL155208 54960 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
1353 8692 93 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
3559 8692 93 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
86 8692 93 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
CHEMBL54 8692 93 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
DB00502 8692 93 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
103 10925 61 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 10925 61 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 10925 61 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 10925 61 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 10925 61 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
10379766 11678 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.2 CCc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
CHEMBL104571 11678 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.2 CCc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
17755999 149663 1 None -5 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 149663 1 None -5 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
86767097 136207 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 359 3 1 5 4.5 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671286 136207 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 359 3 1 5 4.5 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
135398737 7745 93 None -44 90 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 7745 93 None -44 90 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 7745 93 None -44 90 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 7745 93 None -44 90 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 7745 93 None -44 90 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
10472143 126055 0 None -645 16 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 126055 0 None -645 16 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
11777127 32582 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 32582 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
228 7233 28 None -35 23 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
33 7233 28 None -35 23 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
6005 7233 28 None -35 23 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
CHEMBL53 7233 28 None -35 23 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
DB00714 7233 28 None -35 23 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
10154 148907 59 None -58 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL388342 148907 59 None -58 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
9980998 37808 0 None -1819 7 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL139926 37808 0 None -1819 7 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL2112911 37808 0 None -1819 7 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
11697270 84085 0 None -3467 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
CHEMBL208274 84085 0 None -3467 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
44340376 117423 0 None -24 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 117423 0 None -24 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25256816 188387 0 None -4466 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 188387 0 None -4466 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
16754 92349 50 None -67 7 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL228082 92349 50 None -67 7 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
25139181 191121 0 None -1513 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 191121 0 None -1513 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
44567587 185014 0 None -66 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL465055 185014 0 None -66 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
127046951 146680 0 None -61 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 146680 0 None -61 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137633705 163397 0 None -5370 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 163397 0 None -5370 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
122177645 127991 0 None -13803 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 127991 0 None -13803 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
57391897 76084 0 None -301 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 76084 0 None -301 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
57393634 76094 0 None -26 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 76094 0 None -26 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
24824063 104777 11 None -5 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cc4ccccn4n3)CC2)cc1 10.1021/jm701375u
CHEMBL272853 104777 11 None -5 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cc4ccccn4n3)CC2)cc1 10.1021/jm701375u
44381216 127110 0 None -19054 4 Bovine 4.5 pKi = 4.5 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 127110 0 None -19054 4 Bovine 4.5 pKi = 4.5 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
44329314 214721 0 None -69 3 Bovine 4.5 pKi = 4.5 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL96958 214721 0 None -69 3 Bovine 4.5 pKi = 4.5 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
154706546 183225 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4452329 183225 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596339 183225 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
17755991 159077 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 159077 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
96918 19262 30 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
CHEMBL1186488 19262 30 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
118711257 120732 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccccc1CNc1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
CHEMBL3325907 120732 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccccc1CNc1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
44568534 181095 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 265 0 2 3 2.6 CN1CCc2cc(N)cc3c2[C@H]1Cc1cccc(N)c1-3 10.1016/j.bmc.2008.05.077
CHEMBL455051 181095 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 265 0 2 3 2.6 CN1CCc2cc(N)cc3c2[C@H]1Cc1cccc(N)c1-3 10.1016/j.bmc.2008.05.077
10438027 72962 0 None -954 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 72962 0 None -954 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
44415805 88310 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 561 4 1 5 7.1 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(CC3CCCCC3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL216047 88310 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 561 4 1 5 7.1 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(CC3CCCCC3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
96918 19262 30 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
CHEMBL1186488 19262 30 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
154704705 183104 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4590356 183104 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 183104 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
10367486 16066 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL110948 16066 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL543613 16066 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
1042 8362 23 None -204 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 8362 23 None -204 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 8362 23 None -204 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 8362 23 None -204 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 8362 23 None -204 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
72708126 98977 0 None -7 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425375 98977 0 None -7 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
71450550 90582 0 None -6 16 Human 5.5 pKi = 5.5 Binding
Binding affinity to D1 dopamine receptorBinding affinity to D1 dopamine receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 90582 0 None -6 16 Human 5.5 pKi = 5.5 Binding
Binding affinity to D1 dopamine receptorBinding affinity to D1 dopamine receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
736083 168993 17 None -50 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL416288 168993 17 None -50 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
10452020 125053 3 None 10 3 Human 8.5 pKi = 8.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm9800292
CHEMBL34095 125053 3 None 10 3 Human 8.5 pKi = 8.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm9800292
10516818 32423 0 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135197 32423 0 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
122324 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
6077 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
CHEMBL86931 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
10467946 55243 4 None -1 4 Bovine 8.5 pKi = 8.5 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
CHEMBL155596 55243 4 None -1 4 Bovine 8.5 pKi = 8.5 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
14809027 113806 0 None 257 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 113806 0 None 257 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 6993 22 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
44415690 86912 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL213336 86912 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415690 86912 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 86912 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
44415506 87014 0 None 169 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL213793 87014 0 None 169 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
46231845 207512 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 207512 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
1153 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
12668023 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
30026874 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
30026875 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
3341 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
6603851 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
933 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
939 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
985 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL1160786 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL1161520 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL588 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
DB00800 8409 58 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
44401164 76591 0 None -19 9 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 76591 0 None -19 9 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
11573628 81474 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 81474 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
46231848 207317 0 None 8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 207317 0 None 8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3038603 108642 8 None 2 3 Human 8.5 pKi = 8.5 Binding
The compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligandThe compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 108642 8 None 2 3 Human 8.5 pKi = 8.5 Binding
The compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligandThe compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
86763997 139251 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697613 139251 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
11778580 72901 1 None -5 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 72901 1 None -5 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
11493746 148101 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 148101 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
17755867 92884 1 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 92884 1 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
44415704 86934 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 86934 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
15937717 27419 0 None 346 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 253 2 1 2 3.4 CCCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL130851 27419 0 None 346 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 253 2 1 2 3.4 CCCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
56944383 118896 0 None -6 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 118896 0 None -6 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
9861622 206223 5 None 1202 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 10.1021/jm00128a038
CHEMBL59139 206223 5 None 1202 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 10.1021/jm00128a038
44415723 148558 0 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL386122 148558 0 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6917970 10463 61 None -1 33 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
8370 10463 61 None -1 33 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
CHEMBL487387 10463 61 None -1 33 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
11079319 138578 1 None -7 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 1 0 4 3.9 CN1CCN(C2=Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm0309811
CHEMBL369367 138578 1 None -7 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 1 0 4 3.9 CN1CCN(C2=Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm0309811
5249956 80170 1 None -4 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL201525 80170 1 None -4 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
44415536 145408 0 None 95 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(I)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL377584 145408 0 None 95 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(I)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
117774127 139201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697564 139201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
142405812 187782 0 None -40 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 381 3 1 4 5.6 CCOc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4758966 187782 0 None -40 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 381 3 1 4 5.6 CCOc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
15937730 25723 0 None 478 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 301 1 1 2 3.9 CN1CCc2cc(Cl)c(O)cc2C(C2C=CC=CC=C2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL128649 25723 0 None 478 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 301 1 1 2 3.9 CN1CCc2cc(Cl)c(O)cc2C(C2C=CC=CC=C2)C1 10.1016/S0960-894X(00)80155-9
44439945 100142 0 None 1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245571 100142 0 None 1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
71474025 152105 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 152105 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
71474025 152105 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 152105 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
44561317 195753 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 1 2 3.4 CCN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL508399 195753 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 1 2 3.4 CCN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
44415593 87022 0 None -3 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 87022 0 None -3 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6603703 6996 10 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
9637 6996 10 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
CHEMBL291143 6996 10 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
12668019 17011 8 None 204 3 Human 7.5 pKi = 7.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/jm9800292
CHEMBL1160787 17011 8 None 204 3 Human 7.5 pKi = 7.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/jm9800292
44415338 162535 0 None 69 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 579 3 1 7 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnn(-c4ccccc4)c3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL405751 162535 0 None 69 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 579 3 1 7 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnn(-c4ccccc4)c3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6603703 6996 10 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
9637 6996 10 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
CHEMBL291143 6996 10 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
74223723 136193 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 334 3 1 4 4.6 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671272 136193 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 334 3 1 4 4.6 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
44320378 212842 0 None 25 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85409 212842 0 None 25 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764212 139226 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 4 4.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697589 139226 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 4 4.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
9949441 121239 0 None -7 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL333455 121239 0 None -7 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
53364155 70618 0 None -27 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803026 70618 0 None -27 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
71733932 97827 0 None -416 6 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2397389 97827 0 None -416 6 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
145988693 173945 0 None -12 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 173945 0 None -12 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
10310103 114089 0 None -776 9 Rat 5.5 pKi = 5.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 114089 0 None -776 9 Rat 5.5 pKi = 5.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
3038495 7495 37 None -2041 18 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
7625 7495 37 None -2041 18 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
CHEMBL25236 7495 37 None -2041 18 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
44436600 98577 0 None -3019 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 98577 0 None -3019 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
44340227 117418 0 None -2137 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 117418 0 None -2137 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10663221 40487 1 None -60 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
CHEMBL142217 40487 1 None -60 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
11983282 145721 0 None -5128 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 145721 0 None -5128 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
10333195 54960 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
CHEMBL155208 54960 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
25128757 110081 0 None -831 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 110081 0 None -831 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
44448058 161983 0 None 2 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL402517 161983 0 None 2 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
72545007 99897 0 None -199 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 99897 0 None -199 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
24824060 162494 0 None -12 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
CHEMBL405292 162494 0 None -12 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
10404663 173640 10 None -1000 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL428561 173640 10 None -1000 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
12050198 207033 0 None -87 4 Bovine 4.5 pKi = 4.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59702 207033 0 None -87 4 Bovine 4.5 pKi = 4.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
156012196 184111 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4637246 184111 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
46227242 206709 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 2 1 2 3.5 Cc1ccccc1CC1c2ccc(O)cc2CCN1C 10.1016/j.bmc.2009.08.028
CHEMBL594798 206709 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 2 1 2 3.5 Cc1ccccc1CC1c2ccc(O)cc2CCN1C 10.1016/j.bmc.2009.08.028
10809507 126462 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(OC)cc(Br)c2C1Cc1ccccc1O 10.1021/jm991034o
CHEMBL347243 126462 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(OC)cc(Br)c2C1Cc1ccccc1O 10.1021/jm991034o
76314268 113211 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 113211 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 113211 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
188249 46427 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL147463 46427 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL2022280 46427 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
15654862 210430 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ccncc32)CC1 10.1021/jm00067a009
CHEMBL67298 210430 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ccncc32)CC1 10.1021/jm00067a009
15654863 210216 0 None 7 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ccncc32)CC1 10.1021/jm00067a009
CHEMBL65768 210216 0 None 7 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ccncc32)CC1 10.1021/jm00067a009
15654861 107518 0 None 3 2 Rat 4.5 pKi = 4.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ncccc32)CC1 10.1021/jm00067a009
CHEMBL292738 107518 0 None 3 2 Rat 4.5 pKi = 4.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ncccc32)CC1 10.1021/jm00067a009
44591099 182969 0 None -1122 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459350 182969 0 None -1122 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
9796958 153356 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL2115374 153356 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL39230 153356 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL544814 153356 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL3215298 218010 13 None -6 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(C=C[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(C=C[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
681 8247 72 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
940 8247 72 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
947 8247 72 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
CHEMBL59 8247 72 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
DB00988 8247 72 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
10474964 137249 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 137249 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 137249 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
10693836 16109 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL111189 16109 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL545488 16109 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
44579031 196614 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 391 8 0 3 6.1 CCCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL516580 196614 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 391 8 0 3 6.1 CCCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415835 146572 0 None 181 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL379875 146572 0 None 181 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
45271622 20803 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197278 20803 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL564909 20803 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
134147903 156206 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 383 6 2 5 4.3 CCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3945856 156206 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 383 6 2 5 4.3 CCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
9949441 121239 0 None -7 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL333455 121239 0 None -7 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
117774096 139208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 5 3.7 Cc1cc(Oc2ncccc2C(C)C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697571 139208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 5 3.7 Cc1cc(Oc2ncccc2C(C)C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
135398737 7745 93 None -44 90 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
38 7745 93 None -44 90 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
722 7745 93 None -44 90 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
CHEMBL42 7745 93 None -44 90 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
DB00363 7745 93 None -44 90 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
64638 112918 2 None 40 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 112918 2 None 40 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44320053 212552 0 None 257 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 212552 0 None 257 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44319976 113740 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
CHEMBL315005 113740 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
11186895 94282 25 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334885 94282 25 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
242 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
242 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 7258 124 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
44436599 98576 0 None -257 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241211 98576 0 None -257 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
136043855 148306 0 None -389 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 482 2 1 6 5.6 FC1(F)Oc2cccc(CN3CCN(C4=Nc5cc(Cl)ccc5Nc5ccccc54)CC3)c2O1 10.1016/j.bmcl.2006.06.034
CHEMBL384634 148306 0 None -389 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 482 2 1 6 5.6 FC1(F)Oc2cccc(CN3CCN(C4=Nc5cc(Cl)ccc5Nc5ccccc54)CC3)c2O1 10.1016/j.bmcl.2006.06.034
127031949 145533 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 317 7 2 5 2.8 COc1cc(CCN(C)Cc2cccc(O)c2OC)ccc1O 10.1016/j.bmc.2016.03.037
CHEMBL3780438 145533 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 317 7 2 5 2.8 COc1cc(CCN(C)Cc2cccc(O)c2OC)ccc1O 10.1016/j.bmc.2016.03.037
4189 213701 96 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
117773625 139191 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.4 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2)c(C)c(=O)[nH]c1=O nan
CHEMBL3697554 139191 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.4 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2)c(C)c(=O)[nH]c1=O nan
44319988 212858 0 None 3 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85552 212858 0 None 3 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
156012433 184093 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 326 2 1 5 3.1 COc1cc2c3c(c1O)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636948 184093 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 326 2 1 5 3.1 COc1cc2c3c(c1O)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
3246545 209253 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 209253 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 209253 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
44319915 212744 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84557 212744 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44415848 86684 0 None 40 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212438 86684 0 None 40 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
134150852 158474 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 461 6 2 5 5.1 CCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3964242 158474 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 461 6 2 5 5.1 CCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
86764320 139247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697609 139247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
15711869 20112 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1192194 20112 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL543390 20112 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
6852376 98374 13 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL1467585 98374 13 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL24077 98374 13 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL503958 98374 13 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
71109986 157412 0 None - 1 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
CHEMBL3955446 157412 0 None - 1 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
54585811 68384 0 None -2454 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771113 68384 0 None -2454 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
49783042 24463 0 None -112 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258495 24463 0 None -112 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
10871118 213586 0 None -489 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
CHEMBL90374 213586 0 None -489 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
10667043 35322 0 None 7 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 7 2 3 4.6 NCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137637 35322 0 None 7 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 7 2 3 4.6 NCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
44537929 204859 0 None -53 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(O)c(Cl)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574296 204859 0 None -53 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(O)c(Cl)cc21 10.1016/j.bmc.2009.05.079
2470 10425 50 None -4168 58 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
3300 10425 50 None -4168 58 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
5265 10425 50 None -4168 58 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
99 10425 50 None -4168 58 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
CHEMBL267930 10425 50 None -4168 58 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
15021876 110187 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm00111a046
CHEMBL308480 110187 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm00111a046
15021876 110187 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm981094e
CHEMBL308480 110187 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm981094e
10093238 214396 0 None -1 3 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 414 8 0 5 3.9 O=C(CCCN1CCN(CCC2Cc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL95112 214396 0 None -1 3 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 414 8 0 5 3.9 O=C(CCCN1CCN(CCC2Cc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
10738913 211742 0 None -5 5 Rat 4.5 pKi = 4.5 Binding
Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.
ChEMBL 386 8 2 5 1.5 CCOC(=O)c1[nH]c2ccc(CCN3C(=O)CNC3=O)cc2c1CCN(C)C 10.1021/jm9605849
CHEMBL76480 211742 0 None -5 5 Rat 4.5 pKi = 4.5 Binding
Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.
ChEMBL 386 8 2 5 1.5 CCOC(=O)c1[nH]c2ccc(CCN3C(=O)CNC3=O)cc2c1CCN(C)C 10.1021/jm9605849
73356845 98979 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425377 98979 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
235224 134933 29 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
CHEMBL36654 134933 29 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
45481864 204913 0 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 2 2 3.5 Oc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574695 204913 0 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 2 2 3.5 Oc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
2402 10143 62 None -61 24 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 10143 62 None -61 24 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 10143 62 None -61 24 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 10143 62 None -61 24 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 10143 62 None -61 24 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
44320328 213007 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
CHEMBL86669 213007 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
11696813 194697 12 None -316 9 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
CHEMBL496739 194697 12 None -316 9 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
73356845 98979 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425377 98979 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
6603820 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
6603820 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL25856 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
15937720 123652 0 None 81 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 271 2 1 3 3.3 CCSC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL338237 123652 0 None 81 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 271 2 1 3 3.3 CCSC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
86763999 139254 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.5 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2C)n(C)c(=O)[nH]c1=O nan
CHEMBL3697616 139254 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.5 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2C)n(C)c(=O)[nH]c1=O nan
45483269 203738 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 426 4 0 7 4.1 CSc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
CHEMBL566508 203738 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 426 4 0 7 4.1 CSc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
44396220 132201 1 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 132201 1 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
90666899 116222 0 None -6 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
CHEMBL3220215 116222 0 None -6 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
2865 10915 73 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 10915 73 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 10915 73 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 10915 73 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 10915 73 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
511482 104027 6 None -251 5 Bovine 6.5 pKi = 6.5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268799 104027 6 None -251 5 Bovine 6.5 pKi = 6.5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
46917637 75107 0 None -275 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 75107 0 None -275 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
44417647 88936 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 88936 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 88936 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
44400519 139907 0 None -549 5 Pig 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 139907 0 None -549 5 Pig 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10438027 72962 0 None -1096 6 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
CHEMBL184383 72962 0 None -1096 6 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
44381147 65503 0 None -93 4 Bovine 5.5 pKi = 5.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168544 65503 0 None -93 4 Bovine 5.5 pKi = 5.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
44340415 15350 0 None -3 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 15350 0 None -3 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340333 16434 0 None -1071 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 16434 0 None -1071 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
122181330 128649 0 None -3890 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 128649 0 None -3890 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
44372153 126942 0 None -89 4 Bovine 5.5 pKi = 5.5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL351550 126942 0 None -89 4 Bovine 5.5 pKi = 5.5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
71734127 97832 0 None -6760 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397476 97832 0 None -6760 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
10247561 104780 0 None -3 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL272873 104780 0 None -3 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
118711252 120727 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(N)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325901 120727 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(N)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
71562965 94349 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
CHEMBL2335739 94349 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
24829343 165800 0 None -4265 9 Human 5.5 pKi = 5.5 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 165800 0 None -4265 9 Human 5.5 pKi = 5.5 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
112500031 139246 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 0 5 4.3 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697608 139246 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 0 5 4.3 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)cnc(=O)n1C nan
70682090 82844 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057451 82844 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70682090 82844 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057451 82844 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
72708128 98980 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425378 98980 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
11154555 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
2105 9828 37 None -123 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 9828 37 None -123 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 9828 37 None -123 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 9828 37 None -123 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 9828 37 None -123 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
86764215 139235 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697597 139235 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
10537185 32457 0 None -12 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135224 32457 0 None -12 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
86767087 136194 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 318 3 1 4 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnn1C nan
CHEMBL3671273 136194 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 318 3 1 4 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnn1C nan
9948254 115046 0 None -141 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm00402a024
CHEMBL31973 115046 0 None -141 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm00402a024
15115515 115383 0 None -47 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL320526 115383 0 None -47 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
167715 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
969 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
CHEMBL225230 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
53317727 64717 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 313 3 1 3 3.5 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
CHEMBL1672313 64717 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 313 3 1 3 3.5 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
11121216 36912 0 None -169 14 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 36912 0 None -169 14 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
167715 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
969 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
CHEMBL225230 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
44395741 188360 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL476935 188360 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL558392 188360 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
56597938 10712 3 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 10712 3 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 10712 3 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
167715 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
969 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
CHEMBL225230 9651 14 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
44454734 104503 0 None -912 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL271513 104503 0 None -912 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
25130816 194490 0 None -20 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 490 8 2 5 5.8 CCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL495327 194490 0 None -20 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 490 8 2 5 5.8 CCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
45483654 204897 0 None -14 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
CHEMBL574569 204897 0 None -14 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
2779264 118119 38 None -30 4 Bovine 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL326877 118119 38 None -30 4 Bovine 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
42605994 24646 0 None -16 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 24646 0 None -16 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
11566745 81469 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 81469 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 81469 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
167715 9651 14 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
969 9651 14 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
CHEMBL225230 9651 14 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
11154555 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 7587 62 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7077 73733 27 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 73733 27 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL3925724 73733 27 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
3158 63041 27 None -2398 20 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 63041 27 None -2398 20 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
72708128 98980 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425378 98980 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
117774393 139236 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 307 3 1 4 3.5 Cc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c1 nan
CHEMBL3697598 139236 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 307 3 1 4 3.5 Cc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c1 nan
44588898 19375 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186959 19375 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL484352 19375 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
25256815 196333 0 None -51 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 397 6 0 3 3.9 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL514382 196333 0 None -51 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 397 6 0 3 3.9 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2009.01.067
10833201 175390 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 373 2 0 3 4.7 CCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL436042 175390 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 373 2 0 3 4.7 CCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
10707972 175835 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
CHEMBL439639 175835 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
72708127 98978 0 None -40 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425376 98978 0 None -40 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
13091359 120316 0 None -489 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 120316 0 None -489 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
112500033 139249 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697611 139249 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)cnc(=O)n1C nan
118711265 120736 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 345 2 2 3 4.4 CN1CCc2cc(-c3ccc(O)cc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325916 120736 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 345 2 2 3 4.4 CN1CCc2cc(-c3ccc(O)cc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
44415551 87084 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL214142 87084 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
2726 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
621 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
83 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
CHEMBL71 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
DB00477 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
6852376 98374 13 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL1467585 98374 13 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL24077 98374 13 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL503958 98374 13 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
2726 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
621 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
83 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
CHEMBL71 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
DB00477 7706 68 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
10402378 72899 0 None -19 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 72899 0 None -19 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
86764105 139260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 3 1 5 3.6 Cc1cc(Sc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697623 139260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 3 1 5 3.6 Cc1cc(Sc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
6603820 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 102549 19 None -4 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
90140110 136216 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cn[nH]c(=O)c1C nan
CHEMBL3671294 136216 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cn[nH]c(=O)c1C nan
70690499 82846 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057453 82846 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
70690499 82846 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.12.016
CHEMBL2057453 82846 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.12.016
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
24882561 102116 0 None -2041 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL256637 102116 0 None -2041 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
44403225 77323 0 None -346 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194755 77323 0 None -346 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
44436596 98771 1 None -436 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241631 98771 1 None -436 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
10707972 175835 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
CHEMBL439639 175835 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
44567588 197006 0 None -45 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 325 3 2 4 3.6 CCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL517491 197006 0 None -45 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 325 3 2 4 3.6 CCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
90644230 118567 0 None -1819 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 118567 0 None -1819 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
10479188 209652 0 None -316 4 Bovine 5.5 pKi = 5.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62602 209652 0 None -316 4 Bovine 5.5 pKi = 5.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44319370 113824 0 None -1 4 Bovine 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 113824 0 None -1 4 Bovine 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
44380717 127127 0 None -138 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353087 127127 0 None -138 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
56926587 75785 0 None -2290 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
CHEMBL1923416 75785 0 None -2290 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
118711253 120728 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(O)c(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325903 120728 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(O)c(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
112500030 139245 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697607 139245 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
135398737 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
38 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
722 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
CHEMBL42 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
DB00363 7745 93 None -83 90 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
1353 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
3559 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
86 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
CHEMBL54 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
DB00502 8692 93 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
681 8247 72 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
135398745 9688 112 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
117772904 139197 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 5 3.0 Cc1cc(Oc2nccc(C)c2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697560 139197 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 5 3.0 Cc1cc(Oc2nccc(C)c2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90666903 116226 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
CHEMBL3220219 116226 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
155552185 180840 0 None -660 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None -660 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
118709173 120198 0 None -218 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318846 120198 0 None -218 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
72545240 99904 0 None -229 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 99904 0 None -229 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
52937777 67945 0 None -6165 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL1765630 67945 0 None -6165 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
57395340 76075 0 None -407 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 76075 0 None -407 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
71734029 97830 0 None -10964 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397392 97830 0 None -10964 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
14198593 205453 1 None 4 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 205453 1 None 4 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
10064053 102682 0 None -1995 6 Rat 5.4 pKi = 5.4 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 311 1 0 1 5.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(-c2ccccc2)c1-3 10.1021/jm960189i
CHEMBL25924 102682 0 None -1995 6 Rat 5.4 pKi = 5.4 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 311 1 0 1 5.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(-c2ccccc2)c1-3 10.1021/jm960189i
10546334 72020 0 None -2187 5 Human 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 358 4 2 4 4.0 c1ccc2c(N3CCN(CCc4ccc5c(c4)NCN5)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
CHEMBL182721 72020 0 None -2187 5 Human 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 358 4 2 4 4.0 c1ccc2c(N3CCN(CCc4ccc5c(c4)NCN5)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
57580939 98976 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425374 98976 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
154726529 183224 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4467486 183224 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596338 183224 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
15711870 19728 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1189332 19728 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL538520 19728 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
154704418 183366 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4546749 183366 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 183366 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
44567688 199054 0 None -8 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 295 2 1 3 3.5 CCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
CHEMBL520573 199054 0 None -8 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 295 2 1 3 3.5 CCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
42625293 63023 0 None -912 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 63023 0 None -912 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
3036864 209533 19 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 209533 19 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 209533 19 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 209533 19 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
133 9274 52 None -30 43 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -30 43 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -30 43 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -30 43 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -30 43 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
24847750 189982 9 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/np50094a001
CHEMBL479587 189982 9 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/np50094a001
5281878 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
5281881 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
948 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
968 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
CHEMBL42055 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
CHEMBL54661 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
DB00875 8441 35 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
11777127 32582 0 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 32582 0 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
118711256 120731 0 None -37 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1cccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
CHEMBL3325906 120731 0 None -37 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1cccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
15115516 16540 0 None -1148 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL113527 16540 0 None -1148 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
53317511 64712 0 None -107 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 329 3 2 4 3.2 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
CHEMBL1672308 64712 0 None -107 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 329 3 2 4 3.2 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
44380816 127129 0 None -77 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353090 127129 0 None -77 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44448059 101595 0 None 5 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL253530 101595 0 None 5 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
137655451 165632 0 None -288 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 165632 0 None -288 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
3033769 10054 61 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
3299 10054 61 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
94 10054 61 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
CHEMBL8809 10054 61 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
DB12518 10054 61 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
10544858 176807 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
CHEMBL444269 176807 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
CHEMBL542181 176807 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
228 7233 28 None -35 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
33 7233 28 None -35 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
6005 7233 28 None -35 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
CHEMBL53 7233 28 None -35 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
DB00714 7233 28 None -35 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
16573 184398 34 None -18 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 184398 34 None -18 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
44320267 212991 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 212991 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44278297 105852 0 None -2511 3 Rat 4.4 pKi = 4.4 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 382 4 0 2 5.0 O=C(c1cccc(CN2CCC(c3ccc(Cl)cc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
CHEMBL280534 105852 0 None -2511 3 Rat 4.4 pKi = 4.4 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 382 4 0 2 5.0 O=C(c1cccc(CN2CCC(c3ccc(Cl)cc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
130442557 173852 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4289538 173852 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
71110287 153103 0 None - 1 Human 6.4 pKi = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3921127 153103 0 None - 1 Human 6.4 pKi = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
235224 134933 29 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
CHEMBL36654 134933 29 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
72708127 98978 0 None -40 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425376 98978 0 None -40 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
44396235 175316 1 None -23 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 175316 1 None -23 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
72699718 121972 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 355 3 1 4 4.5 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CCC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344465 121972 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 355 3 1 4 4.5 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CCC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
135458464 87903 0 None -1122 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 486 3 1 5 6.2 FC(F)(F)Oc1cccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c1 10.1016/j.bmcl.2006.06.034
CHEMBL215669 87903 0 None -1122 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 486 3 1 5 6.2 FC(F)(F)Oc1cccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c1 10.1016/j.bmcl.2006.06.034
46231783 207312 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 357 1 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C(=O)O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598915 207312 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 357 1 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C(=O)O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
130442473 174116 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4294397 174116 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
86764318 139238 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 349 4 1 5 3.1 Cc1c(-c2ccc(Oc3ncccc3C3CC3)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697600 139238 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 349 4 1 5 3.1 Cc1c(-c2ccc(Oc3ncccc3C3CC3)cc2)n(C)c(=O)[nH]c1=O nan
117773358 139195 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 3 1 5 4.2 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697558 139195 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 3 1 5 4.2 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
23625925 100346 0 None -18 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
CHEMBL246484 100346 0 None -18 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
10436653 39566 1 None -562 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
CHEMBL141419 39566 1 None -562 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
147230103 186932 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2020.127563
CHEMBL4748915 186932 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2020.127563
53327908 68383 0 None -3162 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771112 68383 0 None -3162 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
3082625 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL53510 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
53327665 73254 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL1852240 73254 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL3216759 73254 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
128434 202485 8 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 227 1 3 3 2.2 NCC1c2ccccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
CHEMBL55693 202485 8 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 227 1 3 3 2.2 NCC1c2ccccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
10386748 111529 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
CHEMBL310734 111529 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
10386748 111529 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL310734 111529 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
53363199 70626 0 None -457 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803051 70626 0 None -457 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
25139477 191024 0 None -870 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL483593 191024 0 None -870 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
49782603 24261 0 None -151 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257811 24261 0 None -151 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
137634397 162884 0 None -11748 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 162884 0 None -11748 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
10802235 20031 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1191487 20031 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL542593 20031 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
72545238 99902 0 None -7413 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 99902 0 None -7413 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
112500028 139243 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697605 139243 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)ncc(=O)n1C nan
56971032 76024 0 None -114 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccccn1 10.1016/j.ejmech.2011.11.023
CHEMBL1927094 76024 0 None -114 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccccn1 10.1016/j.ejmech.2011.11.023
3082625 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
CHEMBL53510 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
3082625 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL53510 201507 8 None -199 4 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
44582675 196480 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 196480 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
10786190 121510 0 None -50 3 Rat 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 383 2 0 4 3.7 CN1CCc2cccc3c2[C@H]1Cc1cccc(OS(=O)(=O)C(F)(F)F)c1-3 10.1021/jm960189i
CHEMBL333836 121510 0 None -50 3 Rat 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 383 2 0 4 3.7 CN1CCc2cccc3c2[C@H]1Cc1cccc(OS(=O)(=O)C(F)(F)F)c1-3 10.1021/jm960189i
44406003 139936 0 None 4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
CHEMBL370364 139936 0 None 4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
448537 167029 89 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 167029 89 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
10813037 53931 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 439 3 1 3 4.7 COc1ccc(Br)c(CC2c3c(O)ccc(Br)c3CCN2C)c1 10.1021/jm991034o
CHEMBL154301 53931 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 439 3 1 3 4.7 COc1ccc(Br)c(CC2c3c(O)ccc(Br)c3CCN2C)c1 10.1021/jm991034o
90644059 118807 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 118807 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
10781204 126827 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 309 3 0 3 4.4 CCCN1CCc2cccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL350457 126827 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 309 3 0 3 4.4 CCCN1CCc2cccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
76321556 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
76325150 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
44415658 148350 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 527 3 1 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3sccc3-c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL384916 148350 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 527 3 1 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3sccc3-c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
25110706 19376 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1186960 19376 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
CHEMBL484356 19376 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
86767096 136206 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C#N nan
CHEMBL3671285 136206 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C#N nan
2337 10030 77 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 10030 77 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 10030 77 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 10030 77 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 10030 77 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
44276572 103423 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL26365 103423 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
53364225 70619 0 None -117 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803027 70619 0 None -117 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
30133 74412 8 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
CHEMBL190519 74412 8 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
CHEMBL541862 74412 8 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
10667966 63934 0 None -2 4 Bovine 5.4 pKi = 5.4 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL164736 63934 0 None -2 4 Bovine 5.4 pKi = 5.4 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
44412182 84041 0 None -3890 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL208018 84041 0 None -3890 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
122177642 127988 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 127988 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
24823921 104672 0 None -21 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
CHEMBL272395 104672 0 None -21 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
9995378 12245 0 None -301 4 Bovine 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL107529 12245 0 None -301 4 Bovine 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
10359539 65828 10 None -125 4 Bovine 4.4 pKi = 4.4 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169459 65828 10 None -125 4 Bovine 4.4 pKi = 4.4 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
91899759 136223 0 None - 1 Human 6.4 pKi = 6.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 342 3 1 6 3.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1C#N nan
CHEMBL3671300 136223 0 None - 1 Human 6.4 pKi = 6.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 342 3 1 6 3.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1C#N nan
57580939 98976 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425374 98976 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
1242 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
1242 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
935 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
CHEMBL286080 10385 27 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
10333837 120311 0 None -51 3 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 0 2 3.8 COc1c(C)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL332178 120311 0 None -51 3 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 0 2 3.8 COc1c(C)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
25130157 110084 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 110084 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
135409492 175949 50 None -4 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
CHEMBL440512 175949 50 None -4 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
15467370 109095 0 None -3630 4 Bovine 4.4 pKi = 4.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL303538 109095 0 None -3630 4 Bovine 4.4 pKi = 4.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
76321556 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 113154 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
151086 98753 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
CHEMBL2414991 98753 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
3802 209802 21 None -19 5 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
CHEMBL63329 209802 21 None -19 5 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
3802 209802 21 None -19 5 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm00067a009
CHEMBL63329 209802 21 None -19 5 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm00067a009
4302960 107838 63 None -1258 6 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL294747 107838 63 None -1258 6 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
10247701 92658 0 None -2398 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 4 1 3 4.1 c1ccc2c(N3CCN(CCc4ccc5[nH]cnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
CHEMBL2298806 92658 0 None -2398 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 4 1 3 4.1 c1ccc2c(N3CCN(CCc4ccc5[nH]cnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
162657175 187612 0 None 41 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 331 2 1 3 5.1 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4756987 187612 0 None 41 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 331 2 1 3 5.1 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
16007117 86811 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 86811 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415518 86853 0 None 45 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213084 86853 0 None 45 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415724 87033 0 None 97 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 547 2 1 5 6.4 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cc(Cl)cc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213881 87033 0 None 97 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 547 2 1 5 6.4 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cc(Cl)cc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11637457 79862 1 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 79862 1 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
71562964 94350 0 None 3 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335740 94350 0 None 3 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
37459 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
62 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
CHEMBL8514 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
16007117 86811 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212912 86811 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
15111049 20727 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL1196674 20727 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL557799 20727 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
74223771 136198 0 None - 1 Human 8.4 pKi = 8.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671277 136198 0 None - 1 Human 8.4 pKi = 8.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
86764214 139234 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 4 1 5 4.6 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)(F)F nan
CHEMBL3697596 139234 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 4 1 5 4.6 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)(F)F nan
71109897 94288 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2334893 94288 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 10.1016/j.bmc.2012.12.016
134145434 156188 0 None 173 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 449 5 2 6 3.6 COCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3945691 156188 0 None 173 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 449 5 2 6 3.6 COCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
45379369 14294 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 14294 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
71109897 94288 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
CHEMBL2334893 94288 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
37459 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
62 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
CHEMBL8514 7533 13 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
10518837 107249 0 None 33 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290842 107249 0 None 33 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
46231924 207357 0 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 207357 0 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
5249956 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201525 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
5249956 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
440229 94286 53 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334891 94286 53 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
5249956 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 80170 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
74223826 136215 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671293 136215 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
228 7233 28 None -35 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
33 7233 28 None -35 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
6005 7233 28 None -35 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL53 7233 28 None -35 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
DB00714 7233 28 None -35 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
86767083 136189 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 4 5.3 [C-]#[N+]c1c[nH]c2ccnc(Oc3ccc(-c4c(C)ncnc4C)c(C)c3)c12 nan
CHEMBL3671268 136189 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 4 5.3 [C-]#[N+]c1c[nH]c2ccnc(Oc3ccc(-c4c(C)ncnc4C)c(C)c3)c12 nan
44323851 213753 0 None 3 4 Rat 8.3 pKi = 8.3 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91310 213753 0 None 3 4 Rat 8.3 pKi = 8.3 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
46231770 208089 0 None 213 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NS(C)(=O)=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL604135 208089 0 None 213 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NS(C)(=O)=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
74223772 136200 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671279 136200 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
25110705 19512 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1187785 19512 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL520821 19512 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
146266 107474 8 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL292418 107474 8 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL540857 107474 8 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
11324141 70632 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 303 1 0 5 3.2 CN1CCN(C2=Cn3cccc3Sc3sccc32)CC1 10.1021/jm049629t
CHEMBL180319 70632 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 303 1 0 5 3.2 CN1CCN(C2=Cn3cccc3Sc3sccc32)CC1 10.1021/jm049629t
44386836 69796 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 342 3 0 4 3.6 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
CHEMBL178797 69796 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 342 3 0 4 3.6 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
1153 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
12668023 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
30026874 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
30026875 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
3341 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
6603851 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
933 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
939 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
985 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL1160786 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL1161520 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL588 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
DB00800 8409 58 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
122205438 144178 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 144178 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
71722299 109257 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 109257 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 109257 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
127031398 145585 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 411 8 1 5 5.0 CCCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3781035 145585 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 411 8 1 5 5.0 CCCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
14198584 205048 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL57579 205048 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1016/j.bmc.2009.05.079
86763998 139252 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697614 139252 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
74223832 136229 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
CHEMBL3671306 136229 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
53364083 70628 0 None -28 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803053 70628 0 None -28 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
44339992 115961 0 None -501 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 115961 0 None -501 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
49782841 24424 0 None -2511 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
CHEMBL1258382 24424 0 None -2511 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
137633454 163370 0 None -1230 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4068702 163370 0 None -1230 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
71454405 85200 0 None -30 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL2111528 85200 0 None -30 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44319102 212920 0 None -16 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 212920 0 None -16 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
11631892 84886 0 None -30902 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
CHEMBL210283 84886 0 None -30902 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
151086 98753 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
CHEMBL2414991 98753 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
4011 89183 49 None -64 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
CHEMBL21731 89183 49 None -64 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
118717796 121970 0 None -14 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 4 1 4 4.7 CCC(C)Cc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344462 121970 0 None -14 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 4 1 4 4.7 CCC(C)Cc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
11349297 92655 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 372 5 2 4 2.7 O=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298800 92655 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 372 5 2 4 2.7 O=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
72708060 98972 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425370 98972 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44320123 113860 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL315849 113860 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
72708060 98972 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425370 98972 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
70692801 83338 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062850 83338 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
118709751 120318 0 None -3162 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 120318 0 None -3162 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
156020547 184937 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4649012 184937 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
74223830 136228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671305 136228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
9909648 212352 3 None -134 11 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81330 212352 3 None -134 11 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
71463207 90849 0 None -169 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207636 90849 0 None -169 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
137640203 163741 0 None -54 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 163741 0 None -54 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
10917920 118223 0 None -5128 10 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 118223 0 None -5128 10 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
45482151 204788 0 None -831 4 Pig 5.4 pKi = 5.4 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
CHEMBL573791 204788 0 None -831 4 Pig 5.4 pKi = 5.4 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
44403220 78701 0 None -169 5 Pig 5.4 pKi = 5.4 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL197214 78701 0 None -169 5 Pig 5.4 pKi = 5.4 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
44380921 65103 0 None -11 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168274 65103 0 None -11 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
9977532 117968 1 None -9999 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 117968 1 None -9999 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
71457844 90851 0 None -2137 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 90851 0 None -2137 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44381117 64605 0 None -120 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167032 64605 0 None -120 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
9909648 212352 3 None -134 11 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL81330 212352 3 None -134 11 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
161379 193994 8 None -79 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
CHEMBL492418 193994 8 None -79 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
681 8247 72 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
940 8247 72 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
947 8247 72 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
CHEMBL59 8247 72 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
DB00988 8247 72 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
10085358 116996 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
CHEMBL323771 116996 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
76328713 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3115576 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3139455 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
1816 9318 102 None -323 18 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
4205 9318 102 None -323 18 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
7241 9318 102 None -323 18 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
CHEMBL654 9318 102 None -323 18 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
DB00370 9318 102 None -323 18 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
21119297 98975 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425373 98975 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44299940 107744 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL294186 107744 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
44415535 86925 0 None 42 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213388 86925 0 None 42 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
24900557 205166 0 None -17 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 409 4 1 7 3.4 CNc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
CHEMBL576756 205166 0 None -17 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 409 4 1 7 3.4 CNc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
44393403 71852 0 None -416 6 Pig 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182379 71852 0 None -416 6 Pig 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
135398737 7745 93 None -37 90 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
38 7745 93 None -37 90 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
722 7745 93 None -37 90 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
CHEMBL42 7745 93 None -37 90 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
DB00363 7745 93 None -37 90 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
57393628 76088 0 None -1230 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 76088 0 None -1230 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
135398737 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
38 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
722 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
CHEMBL42 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
DB00363 7745 93 None -204 90 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
44339984 174576 0 None -186 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 174576 0 None -186 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
53362841 70735 0 None -16 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
CHEMBL1806870 70735 0 None -16 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
53328719 73246 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852163 73246 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216980 73246 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
70690651 83336 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]21 10.1016/j.ejmech.2012.07.025
CHEMBL2062848 83336 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]21 10.1016/j.ejmech.2012.07.025
44588932 19380 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186975 19380 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485041 19380 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
68663 34055 23 None -6 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
CHEMBL136711 34055 23 None -6 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
2337 10030 77 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 10030 77 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 10030 77 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 10030 77 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 10030 77 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
1016 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44582140 189277 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 7 0 4 3.3 COc1cccc(N2CCN(CCCCN3CCc4ccccc4C3=O)CC2)c1 10.1016/j.bmcl.2009.01.067
CHEMBL478688 189277 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 7 0 4 3.3 COc1cccc(N2CCN(CCCCN3CCc4ccccc4C3=O)CC2)c1 10.1016/j.bmcl.2009.01.067
44327167 16150 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL111393 16150 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL544319 16150 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
10516949 54693 0 None 2 2 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1cc2c3c(c1)Oc1ccccc1CC3N(C)CC2 10.1021/jm991034o
CHEMBL154948 54693 0 None 2 2 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1cc2c3c(c1)Oc1ccccc1CC3N(C)CC2 10.1021/jm991034o
117774121 139225 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 384 4 1 6 3.0 Cc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C#N)n(C)c(=O)[nH]c1=O nan
CHEMBL3697588 139225 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 384 4 1 6 3.0 Cc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C#N)n(C)c(=O)[nH]c1=O nan
9945168 130443 0 None -3 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 325 2 0 5 3.0 CN1CCN(C2=Cn3c(C=O)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL362060 130443 0 None -3 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 325 2 0 5 3.0 CN1CCN(C2=Cn3c(C=O)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
76325150 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 113199 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
135398737 7745 93 None -83 90 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
38 7745 93 None -83 90 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
722 7745 93 None -83 90 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
CHEMBL42 7745 93 None -83 90 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
DB00363 7745 93 None -83 90 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
124618 205159 7 None 134 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 243 1 4 4 1.9 NCC1c2cc(O)ccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
CHEMBL57672 205159 7 None 134 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 243 1 4 4 1.9 NCC1c2cc(O)ccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
86764319 139242 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697604 139242 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
127047221 146708 0 None -1 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 146708 0 None -1 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
127046950 146823 0 None -23 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 146823 0 None -23 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
25071385 165936 0 None -208 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 165936 0 None -208 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
681 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
940 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
947 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
CHEMBL59 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
DB00988 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
681 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
940 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
947 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
CHEMBL59 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
DB00988 8247 72 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
10333842 105207 1 None -31 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
CHEMBL27559 105207 1 None -31 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
44448070 101668 0 None 3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL254147 101668 0 None 3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 10.1021/jm060959i
25071691 118564 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 118564 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
72545239 99903 0 None -426 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 99903 0 None -426 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
21119297 98975 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425373 98975 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
25186021 194803 0 None -1318 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/jm800689g
CHEMBL497574 194803 0 None -1318 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/jm800689g
10333842 105207 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
CHEMBL27559 105207 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
10333842 105207 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL27559 105207 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
1530 8963 50 None -53 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 8963 50 None -53 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 8963 50 None -53 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 8963 50 None -53 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 8963 50 None -53 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
76328713 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3115576 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3139455 113181 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
71722291 109237 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397385 109237 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040059 109237 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
11712530 194669 0 None -41686 4 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm800689g
CHEMBL496531 194669 0 None -41686 4 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm800689g
135398737 7745 93 None -44 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
38 7745 93 None -44 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
722 7745 93 None -44 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
CHEMBL42 7745 93 None -44 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
DB00363 7745 93 None -44 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
44415849 148191 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 509 3 1 6 5.1 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
CHEMBL384069 148191 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 509 3 1 6 5.1 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
86764104 139259 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697622 139259 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223775 136209 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 316 3 1 4 4.4 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671288 136209 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 316 3 1 4 4.4 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
681 8247 72 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
940 8247 72 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
947 8247 72 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
CHEMBL59 8247 72 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
DB00988 8247 72 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
137657115 166534 0 None -173 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 166534 0 None -173 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
10831251 169952 0 None 4 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL41809 169952 0 None 4 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44340084 15860 0 None -2238 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 15860 0 None -2238 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
25131137 194326 0 None -3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 558 9 2 5 7.4 Nc1nc2c(s1)C[C@@H](N(CCC1CCCCC1)CC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
CHEMBL494509 194326 0 None -3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 558 9 2 5 7.4 Nc1nc2c(s1)C[C@@H](N(CCC1CCCCC1)CC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
681 8247 72 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
940 8247 72 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
947 8247 72 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
CHEMBL59 8247 72 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
DB00988 8247 72 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
70696888 83348 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062860 83348 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
44329039 214916 0 None -56 3 Bovine 4.4 pKi = 4.4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL98072 214916 0 None -56 3 Bovine 4.4 pKi = 4.4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
14198585 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
14198585 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL293158 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00118a012
44320076 213205 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87910 213205 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11282465 199897 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL522746 199897 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
11406615 92678 0 None -162 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 388 5 2 4 4.1 S=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298832 92678 0 None -162 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 388 5 2 4 4.1 S=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
14198585 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 107578 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
14198585 107578 1 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL293158 107578 1 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00129a006
44415759 148466 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 3 1 5 6.5 CC(C)(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL385590 148466 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 3 1 5 6.5 CC(C)(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
681 8247 72 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
940 8247 72 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
947 8247 72 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
CHEMBL59 8247 72 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
DB00988 8247 72 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
44276551 104151 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL26965 104151 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10333842 105207 1 None -31 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmc.2008.08.056
CHEMBL27559 105207 1 None -31 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmc.2008.08.056
10588327 20553 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1195441 20553 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL554571 20553 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
72699903 121976 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)Cl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344469 121976 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)Cl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
122197088 139193 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 362 3 1 5 3.4 [C-]#[N+]c1c(C)ccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697556 139193 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 362 3 1 5 3.4 [C-]#[N+]c1c(C)ccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
71563082 94056 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2331599 94056 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
9908125 126122 0 None -20 4 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
CHEMBL344270 126122 0 None -20 4 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
11016418 112899 0 None -7244 9 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 112899 0 None -7244 9 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
71456046 90850 0 None -2951 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 90850 0 None -2951 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
127045853 146571 0 None -17782 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 146571 0 None -17782 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137655795 165361 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 165361 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
12050201 209653 0 None -31 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL62624 209653 0 None -31 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
44319361 212499 0 None -7 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 212499 0 None -7 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
44264629 104141 0 None -316 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL269576 104141 0 None -316 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
72545011 99901 0 None -3162 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 99901 0 None -3162 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
42606339 24703 0 None -97 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 24703 0 None -97 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
71734126 97829 0 None -4466 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397391 97829 0 None -4466 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
2812 11551 101 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
127027737 144765 0 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 342 6 1 4 2.2 O=C(NCCCN1CCN(c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3764420 144765 0 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 342 6 1 4 2.2 O=C(NCCCN1CCN(c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
44399174 74787 0 None -870 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatumInhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatum
ChEMBL 449 6 0 5 3.0 O=C1C2C3C=CC(C3)C2C(=O)N1OCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm050246k
CHEMBL191226 74787 0 None -870 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatumInhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatum
ChEMBL 449 6 0 5 3.0 O=C1C2C3C=CC(C3)C2C(=O)N1OCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm050246k
44282127 123347 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743804 123347 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL33644 123347 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
3083157 69810 2 None -229 2 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 277 2 1 2 3.7 C=CCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL1788212 69810 2 None -229 2 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 277 2 1 2 3.7 C=CCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
15711852 20111 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192193 20111 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL543389 20111 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
176 7186 66 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
145968810 171817 0 None -120 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 171817 0 None -120 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
15937731 124268 6 None 5 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 211 0 1 2 2.1 CN1CCc2cc(O)c(Cl)cc2CC1 10.1016/S0960-894X(00)80155-9
CHEMBL340006 124268 6 None 5 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 211 0 1 2 2.1 CN1CCc2cc(O)c(Cl)cc2CC1 10.1016/S0960-894X(00)80155-9
24766199 104300 0 None -1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm701045j
CHEMBL270426 104300 0 None -1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm701045j
24766199 104300 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm9015763
CHEMBL270426 104300 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm9015763
44301054 202927 0 None -218 6 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 202927 0 None -218 6 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
25139481 191619 0 None -32 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
CHEMBL485227 191619 0 None -32 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
25186569 183761 0 None -45708 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
CHEMBL462508 183761 0 None -45708 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
122177643 127989 0 None -2884 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 127989 0 None -2884 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
3198 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10803661 117699 0 None -2 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 1 1 3 3.3 CC(=O)c1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL326159 117699 0 None -2 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 1 1 3 3.3 CC(=O)c1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
25141534 63009 0 None -2238 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 63009 0 None -2238 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
76314268 113211 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 113211 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 113211 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
1353 8692 93 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
3559 8692 93 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
86 8692 93 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
CHEMBL54 8692 93 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
DB00502 8692 93 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
10042602 73064 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1016/j.bmcl.2004.06.005
CHEMBL184770 73064 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1016/j.bmcl.2004.06.005
3106 55294 16 None -87 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL15564 55294 16 None -87 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
10042602 73064 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1007/s00044-012-0055-5
CHEMBL184770 73064 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1007/s00044-012-0055-5
10683943 121159 0 None -81 3 Rat 5.3 pKi = 5.3 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 277 1 0 2 3.6 CC(=O)c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL333134 121159 0 None -81 3 Rat 5.3 pKi = 5.3 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 277 1 0 2 3.6 CC(=O)c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
135398745 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
47 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
CHEMBL715 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
DB00334 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
1353 8692 93 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
3559 8692 93 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
86 8692 93 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
CHEMBL54 8692 93 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
DB00502 8692 93 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
46869265 23029 0 None -4 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2012.08.058
CHEMBL1224527 23029 0 None -4 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2012.08.058
44415839 86672 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212402 86672 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415345 88089 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
CHEMBL215885 88089 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
44415517 86852 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213083 86852 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415345 88089 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
CHEMBL215885 88089 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
11186086 70147 0 None -12 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 313 1 0 3 3.2 CN1CCN(C2=Cc3cc(Cl)ccc3Cn3cccc32)CC1 10.1021/jm049629t
CHEMBL179557 70147 0 None -12 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 313 1 0 3 3.2 CN1CCN(C2=Cc3cc(Cl)ccc3Cn3cccc32)CC1 10.1021/jm049629t
45482153 204817 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL574030 204817 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
137644833 164918 0 None -87 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 164918 0 None -87 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
44436606 98772 0 None -1445 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241641 98772 0 None -1445 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
44339992 115961 0 None -501 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 115961 0 None -501 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
9977532 117968 1 None -9999 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 117968 1 None -9999 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
71734129 97836 0 None -10964 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397480 97836 0 None -10964 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
137654675 165413 0 None -1230 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 165413 0 None -1230 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
11652518 172711 0 None -16 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL425064 172711 0 None -16 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
44329090 214805 0 None -26 3 Bovine 4.3 pKi = 4.3 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97436 214805 0 None -26 3 Bovine 4.3 pKi = 4.3 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
134 9292 24 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 9292 24 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 9292 24 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 9292 24 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 9292 24 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
14787976 203759 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56666 203759 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
44320303 170746 0 None 2 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420788 170746 0 None 2 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11358377 209118 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
CHEMBL610449 209118 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
44415646 146556 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 635 4 1 7 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OC(F)(F)O4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL379862 146556 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 635 4 1 7 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OC(F)(F)O4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
10264969 55069 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
CHEMBL155352 55069 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
15696487 170578 1 None 9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420604 170578 1 None 9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
15654858 109077 0 None 2 2 Rat 4.3 pKi = 4.3 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3cccnc3N(C=O)c3ccccc32)CC1 10.1021/jm00067a009
CHEMBL303435 109077 0 None 2 2 Rat 4.3 pKi = 4.3 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3cccnc3N(C=O)c3ccccc32)CC1 10.1021/jm00067a009
44415807 148414 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccccc1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL385295 148414 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccccc1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
15111052 19547 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1187965 19547 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL534678 19547 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
156017805 184605 0 None 5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4643886 184605 0 None 5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
21171 193755 33 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 193755 33 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
46893146 68381 0 None -3981 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 68381 0 None -3981 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363202 70630 0 None -26 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803055 70630 0 None -26 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
122191605 130498 0 None -23 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 130498 0 None -23 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
44319370 113824 0 None -1 4 Bovine 6.3 pKi = 6.3 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 113824 0 None -1 4 Bovine 6.3 pKi = 6.3 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
10264969 55069 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
CHEMBL155352 55069 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
137634397 162884 0 None -11748 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 162884 0 None -11748 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
24824062 162491 0 None -79 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm701375u
CHEMBL405260 162491 0 None -79 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm701375u
44372312 60559 0 None -43 3 Bovine 5.3 pKi = 5.3 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL160396 60559 0 None -43 3 Bovine 5.3 pKi = 5.3 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
11492 44279 61 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
59111271 44279 61 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
CHEMBL145584 44279 61 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
42606573 24618 0 None -81 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 24618 0 None -81 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
136043859 145683 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 430 2 1 4 5.9 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
CHEMBL378301 145683 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 430 2 1 4 5.9 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
10618131 35276 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 354 6 2 4 3.4 CN(C)CCCCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137583 35276 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 354 6 2 4 3.4 CN(C)CCCCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10518820 117177 0 None -31 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 307 2 0 3 3.7 COc1c(C(C)=O)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL324372 117177 0 None -31 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 307 2 0 3 3.7 COc1c(C(C)=O)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
12049521 209970 0 None -13 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64288 209970 0 None -13 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
117773325 139199 0 None - 1 Human 6.3 pKi = 6.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 5 2.7 Cc1cc(Oc2ncccc2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697562 139199 0 None - 1 Human 6.3 pKi = 6.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 5 2.7 Cc1cc(Oc2ncccc2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44582517 188418 0 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.3 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477446 188418 0 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.3 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
154726792 183363 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 183363 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 183363 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
9841398 106295 4 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
CHEMBL28338 106295 4 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
9841398 106295 4 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL28338 106295 4 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276552 106656 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL285924 106656 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
1353 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
44415822 175621 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(F)cc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL437917 175621 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(F)cc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
10409038 92017 0 None -41 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL225853 92017 0 None -41 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
118709176 120201 0 None -34 4 Pig 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318849 120201 0 None -34 4 Pig 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9952858 14326 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL108764 14326 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
9952858 14326 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL108764 14326 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
167715 9651 14 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
969 9651 14 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL225230 9651 14 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
11504230 84992 0 None -870 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 84992 0 None -870 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
10830557 38075 0 None -4 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL140165 38075 0 None -4 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
46905072 16949 0 None -28 2 Human 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL1159663 16949 0 None -28 2 Human 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
25131138 194328 0 None -72 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 480 8 2 6 5.4 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cc3ccccc3o2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494511 194328 0 None -72 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 480 8 2 6 5.4 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cc3ccccc3o2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
49782602 23941 0 None -162 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256169 23941 0 None -162 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
57390117 76074 0 None -346 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 76074 0 None -346 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
70690653 83349 0 None -32 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062861 83349 0 None -32 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
45481890 205795 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 9 2 9 4.4 COc1ccccc1N1CCN(CCCn2cc(CN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL585742 205795 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 9 2 9 4.4 COc1ccccc1N1CCN(CCCn2cc(CN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
228 7233 28 None -35 23 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 7233 28 None -35 23 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 7233 28 None -35 23 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 7233 28 None -35 23 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 7233 28 None -35 23 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
15225750 148163 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 383 1 1 5 3.2 CC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL383869 148163 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 383 1 1 5 3.2 CC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
57391216 76943 0 None -23 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 76943 0 None -23 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44304603 209917 0 None -43 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64139 209917 0 None -43 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
42625211 63013 0 None -81 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627309 63013 0 None -81 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
14138285 151933 6 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
CHEMBL3912178 151933 6 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
5016 115946 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL32145 115946 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL544114 115946 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
74223772 136200 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671279 136200 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
86767101 136214 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 393 4 1 5 4.4 Cc1ncnc(N2CC(F)C2)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671292 136214 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 393 4 1 5 4.4 Cc1ncnc(N2CC(F)C2)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
6852376 98374 13 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL1467585 98374 13 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL24077 98374 13 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL503958 98374 13 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
15711869 20112 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1192194 20112 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL543390 20112 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
15937729 124940 0 None 301 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 277 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL340855 124940 0 None 301 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 277 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCC2)C1 10.1016/S0960-894X(00)80155-9
70690500 82848 0 None - 1 Human 8.3 pKi = 8.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 82848 0 None - 1 Human 8.3 pKi = 8.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
44401164 76591 0 None -19 9 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 76591 0 None -19 9 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
15115525 116467 0 None 134 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 509 4 2 8 5.0 CN1CCc2cc(Br)c(O)cc2C(c2ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc2)C1 10.1021/jm00115a012
CHEMBL322760 116467 0 None 134 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 509 4 2 8 5.0 CN1CCc2cc(Br)c(O)cc2C(c2ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc2)C1 10.1021/jm00115a012
134155502 158207 0 None 20 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 341 3 2 5 3.2 CCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3961827 158207 0 None 20 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 341 3 2 5 3.2 CCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
15696466 11039 0 None 208 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00114a002
CHEMBL100572 11039 0 None 208 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00114a002
44320050 113608 0 None 138 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 113608 0 None 138 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764106 139211 0 None - 1 Human 8.3 pKi = 8.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 4 4.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697574 139211 0 None - 1 Human 8.3 pKi = 8.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 4 4.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
44356291 29507 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 269 1 3 3 2.7 C[C@@]1(N)Cc2cc(O)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm960318v
CHEMBL132766 29507 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 269 1 3 3 2.7 C[C@@]1(N)Cc2cc(O)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm960318v
162643108 188435 0 None 83 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 335 1 1 3 5.0 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4776090 188435 0 None 83 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 335 1 1 3 5.0 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2020.127563
71563083 94347 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335737 94347 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
10742 10389 31 None -2 8 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
1225 10389 31 None -2 8 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
CHEMBL35354 10389 31 None -2 8 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
5290 206812 40 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)C1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL595489 206812 40 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)C1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
46231769 207836 0 None 371 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)C4CC4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL602659 207836 0 None 371 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)C4CC4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
15937718 122011 0 None 48 2 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 251 2 1 2 3.2 C=CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL334728 122011 0 None 48 2 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 251 2 1 2 3.2 C=CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
10732044 91188 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114440 91188 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219804 91188 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
46231771 207759 0 None 107 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL602052 207759 0 None 107 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
11727683 68823 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 345 1 0 4 4.2 CN1CCCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL177455 68823 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 345 1 0 4 4.2 CN1CCCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
6917970 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
8370 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
CHEMBL487387 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
6917970 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
161665 179364 35 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 179364 35 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
2389 10104 118 None -346 66 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
5073 10104 118 None -346 66 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
96 10104 118 None -346 66 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
CHEMBL85 10104 118 None -346 66 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
DB00734 10104 118 None -346 66 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
2726 7706 68 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
621 7706 68 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
83 7706 68 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
CHEMBL71 7706 68 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
DB00477 7706 68 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
71109989 160554 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3982119 160554 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
2407 10145 76 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
59227 10145 76 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
941 10145 76 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
CHEMBL1303 10145 76 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
DB05271 10145 76 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
3716121 90856 16 None -1258 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207643 90856 16 None -1258 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
145986441 173951 0 None -147 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4291172 173951 0 None -147 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
71454294 90852 0 None -1096 7 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 90852 0 None -1096 7 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
1577 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
2537 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5355 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5501 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
643497 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
688272 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
958 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
960 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL196677 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL26 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL267044 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB00391 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB16021 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
1577 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
2537 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5355 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5501 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
643497 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
688272 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
958 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
960 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL196677 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL26 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL267044 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB00391 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB16021 10475 110 None -69 20 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
10827222 13757 1 None -457 5 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligandBinding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 13757 1 None -457 5 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligandBinding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
45481875 204898 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574595 204898 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
10939222 211181 1 None -1000 5 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL71960 211181 1 None -1000 5 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
44415825 87891 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 573 4 1 5 6.8 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccccc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL215641 87891 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 573 4 1 5 6.8 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccccc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44415786 86825 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 549 6 1 5 6.9 CCC(CC)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212966 86825 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 549 6 1 5 6.9 CCC(CC)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
25141538 63015 0 None -2089 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 63015 0 None -2089 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
154705884 183142 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4469584 183142 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 183142 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
11522476 81298 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 81298 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
162660874 188662 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4779001 188662 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
86764103 139215 13 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 139215 13 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
75201899 178695 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 178695 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
44415838 145858 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL378648 145858 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415560 87145 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 4 1 6 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Oc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL214407 87145 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 4 1 6 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Oc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
9883454 120743 0 None -2 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL332600 120743 0 None -2 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
10758745 107209 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 107209 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 107209 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
9883454 120743 0 None -2 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL332600 120743 0 None -2 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
56833378 75108 0 None -281 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 75108 0 None -281 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
10665598 41857 1 None -30 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
CHEMBL143355 41857 1 None -30 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
164609519 191230 0 None -426 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 191230 0 None -426 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
44454685 101828 0 None -63 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
CHEMBL255163 101828 0 None -63 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
44380715 65787 0 None -269 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169222 65787 0 None -269 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
155569483 182978 0 None -154 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 2 2 5 2.9 CCNc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
CHEMBL4593728 182978 0 None -154 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 2 2 5 2.9 CCNc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
14787977 205661 2 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
CHEMBL58422 205661 2 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
14787976 203759 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56666 203759 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
44405965 81788 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 449 5 2 5 3.2 O=c1[nH]c2[nH]c(-c3ccccc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL203362 81788 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 449 5 2 5 3.2 O=c1[nH]c2[nH]c(-c3ccccc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
135398745 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
44320092 168666 0 None 39 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 168666 0 None 39 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
57401820 76936 0 None -6 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 76936 0 None -6 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
135398745 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
47 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
CHEMBL715 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
DB00334 9688 112 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
10592479 107041 0 None 48 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL288846 107041 0 None 48 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
21302490 119582 32 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 119582 32 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 119582 32 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
74223829 136226 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 351 3 1 5 4.5 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1Cl nan
CHEMBL3671303 136226 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 351 3 1 5 4.5 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1Cl nan
70686343 82847 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057454 82847 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
56971028 76020 0 None -3 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 392 8 1 6 2.5 CCOc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1016/j.ejmech.2011.11.023
CHEMBL1927090 76020 0 None -3 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 392 8 1 6 2.5 CCOc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1016/j.ejmech.2011.11.023
15711865 19947 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL1190906 19947 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL541838 19947 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
117774289 139190 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.1 CCc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697553 139190 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.1 CCc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
164585473 191341 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 191341 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44393372 73100 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL184993 73100 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
1257607 162091 2 None 4 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 433 4 0 5 4.2 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL403032 162091 2 None 4 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 433 4 0 5 4.2 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
45268293 202914 0 None -20 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL561123 202914 0 None -20 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10854877 148793 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL38757 148793 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44454711 104295 0 None -3311 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL270408 104295 0 None -3311 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
10001207 172100 0 None -114 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL423440 172100 0 None -114 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44567597 176243 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL442926 176243 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
90644063 118812 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 118812 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
14198596 108420 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 108420 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
135221 151997 5 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3912606 151997 5 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
90644063 118812 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 118812 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
10826687 57723 0 None -4 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1ccc2c(c1)CC1c3c(cccc3O2)CCN1C 10.1021/jm991034o
CHEMBL157799 57723 0 None -4 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1ccc2c(c1)CC1c3c(cccc3O2)CCN1C 10.1021/jm991034o
44569447 185534 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 323 2 0 4 3.4 COc1cc2c3c(c1)-c1c(cccc1OC(C)=O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.11.025
CHEMBL468677 185534 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 323 2 0 4 3.4 COc1cc2c3c(c1)-c1c(cccc1OC(C)=O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.11.025
1152279 37509 7 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL1395394 37509 7 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
135398737 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
135398737 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 7745 93 None -44 90 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
228 7233 28 None -30 23 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
33 7233 28 None -30 23 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
6005 7233 28 None -30 23 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
CHEMBL53 7233 28 None -30 23 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
DB00714 7233 28 None -30 23 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
11782988 18413 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118092 18413 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
14198586 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
14198586 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00118a012
CHEMBL60706 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00118a012
14198586 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Compound was evaluated for the binding affinity against dopamine (D1) receptorCompound was evaluated for the binding affinity against dopamine (D1) receptor
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 208612 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Compound was evaluated for the binding affinity against dopamine (D1) receptorCompound was evaluated for the binding affinity against dopamine (D1) receptor
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
11782988 18413 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118092 18413 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
86767100 131216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)c(F)c1F nan
CHEMBL3639701 131216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)c(F)c1F nan
44320256 213092 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87172 213092 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
188442 94284 5 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3O)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334887 94284 5 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3O)C[C@@H]21 10.1016/j.bmc.2012.12.016
15467371 107784 0 None -912 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294458 107784 0 None -912 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
10831735 38529 0 None -2511 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140594 38529 0 None -2511 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
10567430 126071 1 None -1445 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL343880 126071 1 None -1445 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
44340097 16212 0 None -4365 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 16212 0 None -4365 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
44567595 182056 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL457275 182056 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
137645830 164631 0 None -131 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 164631 0 None -131 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
11615489 76218 1 None -588 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL193337 76218 1 None -588 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
14787976 203759 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00170a025
CHEMBL56666 203759 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00170a025
14787977 205661 2 None -1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
CHEMBL58422 205661 2 None -1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
156012880 184221 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 364 4 0 5 3.4 C#CCOc1c(OC)cc2c3c1-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4638749 184221 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 364 4 0 5 3.4 C#CCOc1c(OC)cc2c3c1-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
10809188 16047 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL110847 16047 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL540822 16047 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
150 9287 21 None -43 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 9287 21 None -43 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 9287 21 None -43 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 9287 21 None -43 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 9287 21 None -43 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
135398737 7745 93 None -83 90 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
38 7745 93 None -83 90 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
722 7745 93 None -83 90 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
CHEMBL42 7745 93 None -83 90 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
DB00363 7745 93 None -83 90 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
44415824 87987 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 3 1 5 5.5 CCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL215842 87987 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 3 1 5 5.5 CCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
117772871 139258 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697621 139258 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
86767099 136212 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1cc(F)c(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671290 136212 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1cc(F)c(Oc2nccc3[nH]ccc23)cc1F nan
135398737 7745 93 None -44 90 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 7745 93 None -44 90 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 7745 93 None -44 90 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 7745 93 None -44 90 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 7745 93 None -44 90 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
57390118 76077 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 76077 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
12997400 107781 7 None -53 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL294394 107781 7 None -53 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
122132 209343 17 None -87 4 Human 5.3 pKi = 5.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm9800292
CHEMBL611801 209343 17 None -87 4 Human 5.3 pKi = 5.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm9800292
44454735 102092 0 None -2951 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL256492 102092 0 None -2951 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
25131136 194290 0 None -97 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 504 9 2 5 6.2 CCCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494308 194290 0 None -97 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 504 9 2 5 6.2 CCCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
49782837 24357 0 None -44 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1258154 24357 0 None -44 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
137645574 164582 0 None -5754 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 164582 0 None -5754 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
72545009 99899 0 None -109 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 99899 0 None -109 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
145970938 171935 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 171935 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11698732 79520 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccc(Cl)cc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL199876 79520 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccc(Cl)cc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
44304643 210054 0 None -8 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64668 210054 0 None -8 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
3168 16034 92 None -89 22 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -89 22 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
162665267 188961 0 None 21 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.6 CN1CCC(C2=Nc3cc(Cl)ccc3Nc3ccccc32)=CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL4782694 188961 0 None 21 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.6 CN1CCC(C2=Nc3cc(Cl)ccc3Nc3ccccc32)=CC1(C)C 10.1016/j.bmcl.2020.127563
1353 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
117774669 139257 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.0 CCn1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)c(C)c(=O)[nH]c1=O nan
CHEMBL3697620 139257 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.0 CCn1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)c(C)c(=O)[nH]c1=O nan
71454927 91367 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
CHEMBL2158636 91367 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
CHEMBL2221040 91367 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
10641637 125558 0 None -19 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL342001 125558 0 None -19 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
118709172 120196 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318844 120196 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
10336538 8406 50 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
974 8406 50 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
CHEMBL310843 8406 50 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
10336538 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
974 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
CHEMBL310843 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
44436597 98575 0 None -251 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241210 98575 0 None -251 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
11559581 85193 0 None -2754 6 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL211135 85193 0 None -2754 6 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
11654739 183627 0 None -20417 4 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
CHEMBL461236 183627 0 None -20417 4 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
71734031 97835 0 None -22908 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397479 97835 0 None -22908 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
10336538 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
974 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
CHEMBL310843 8406 50 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
10336538 8406 50 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
974 8406 50 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL310843 8406 50 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
44537919 204915 0 None -28 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574700 204915 0 None -28 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
10811026 35320 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 9 2 3 4.3 O=CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137636 35320 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 9 2 3 4.3 O=CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
2398 7741 62 None -11 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 7741 62 None -11 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 7741 62 None -11 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 7741 62 None -11 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 7741 62 None -11 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
6852376 98374 13 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL1467585 98374 13 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL24077 98374 13 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL503958 98374 13 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
44415802 86982 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213668 86982 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415383 88226 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 5 1 6 5.4 COc1ccc(CCC(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1Cl 10.1016/j.bmcl.2006.06.022
CHEMBL215950 88226 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 5 1 6 5.4 COc1ccc(CCC(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1Cl 10.1016/j.bmcl.2006.06.022
25110708 19381 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186978 19381 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485207 19381 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
130442561 173672 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286110 173672 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
44276405 106885 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
CHEMBL287513 106885 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
44412191 145153 0 None -107 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
CHEMBL377200 145153 0 None -107 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
11071135 214787 0 None -2570 8 Rat 5.3 pKi = 5.3 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 214787 0 None -2570 8 Rat 5.3 pKi = 5.3 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
11661609 86468 0 None -5623 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
CHEMBL211539 86468 0 None -5623 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
44339879 179061 0 None -186 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 179061 0 None -186 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
44327153 115987 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
CHEMBL321682 115987 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
CHEMBL558817 115987 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
10738274 171670 0 None -2 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(Br)cc(OC)c2C1Cc1ccccc1O 10.1021/jm991034o
CHEMBL422169 171670 0 None -2 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(Br)cc(OC)c2C1Cc1ccccc1O 10.1021/jm991034o
145982261 173511 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4283176 173511 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
155195311 181126 0 None -1778 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assayDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assay
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acsmedchemlett.9b00660
CHEMBL4551160 181126 0 None -1778 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assayDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assay
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acsmedchemlett.9b00660
24949693 189083 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
CHEMBL478413 189083 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
14198593 205453 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 205453 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
36791366 94279 1 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2334880 94279 1 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
14198593 205453 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL57988 205453 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00118a012
44405985 176339 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccccc3Cl)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL443567 176339 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccccc3Cl)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
122132 209343 17 None 4 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm00160a018
CHEMBL611801 209343 17 None 4 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm00160a018
11720302 173037 0 None -301 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL426863 173037 0 None -301 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
10939167 16272 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 16272 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL129483 16272 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
44454710 162445 0 None -478 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL404888 162445 0 None -478 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
137631036 167930 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4060837 167930 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4117325 167930 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
44415623 145032 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 599 4 1 7 6.4 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL377043 145032 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 599 4 1 7 6.4 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44316058 212316 0 None -64 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80974 212316 0 None -64 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
10316297 130827 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
CHEMBL363124 130827 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
10316297 130827 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
CHEMBL363124 130827 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
53946796 74541 1 None -5248 2 Rat 4.2 pKi = 4.2 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
CHEMBL1907969 74541 1 None -5248 2 Rat 4.2 pKi = 4.2 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
44427970 159389 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 159389 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
156010592 183907 0 None 14 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 376 4 1 4 3.4 C#CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4633772 183907 0 None 14 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 376 4 1 4 3.4 C#CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
86764321 139250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 399 5 1 5 4.3 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C1CC1 nan
CHEMBL3697612 139250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 399 5 1 5 4.3 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C1CC1 nan
117773598 139253 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.7 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2C)c(C)c(=O)[nH]c1=O nan
CHEMBL3697615 139253 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.7 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2C)c(C)c(=O)[nH]c1=O nan
164626655 193372 0 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 193372 0 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
44287454 20000 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1191276 20000 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL542351 20000 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
1353 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
3559 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
86 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
CHEMBL54 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
DB00502 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
2389 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
54580906 68379 0 None -2754 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 68379 0 None -2754 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
57391895 76076 0 None -301 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 76076 0 None -301 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
3156990 14902 22 None -28 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL109173 14902 22 None -28 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
25139478 191735 0 None -446 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL485384 191735 0 None -446 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
15467369 107705 0 None -6165 3 Bovine 4.2 pKi = 4.2 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL293956 107705 0 None -6165 3 Bovine 4.2 pKi = 4.2 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
136043854 86962 0 None -20 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 460 2 1 6 5.1 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc4c(c3)OCCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
CHEMBL213577 86962 0 None -20 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 460 2 1 6 5.1 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc4c(c3)OCCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
77974401 120737 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 252 1 1 2 2.9 CN1CCc2ccc(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325920 120737 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 252 1 1 2 2.9 CN1CCc2ccc(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
154727843 183212 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4448853 183212 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 183212 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
71086428 158332 0 None -66 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3963122 158332 0 None -66 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
3108374 98752 24 None -3 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
CHEMBL2414990 98752 24 None -3 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
107715 207724 22 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
57401819 76935 0 None -75 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 76935 0 None -75 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
23364995 120197 0 None -13 4 Pig 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318845 120197 0 None -13 4 Pig 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
86764104 139259 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697622 139259 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
156020558 184825 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4647167 184825 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
44436617 98335 0 None -20 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL240584 98335 0 None -20 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
49782604 24295 0 None -19 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1257927 24295 0 None -19 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
49782836 24324 0 None -58 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1258036 24324 0 None -58 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
24841480 190678 0 None -2951 20 Human 5.2 pKi = 5.2 Binding
Antagonist activity at dopamine D1 receptor (unknown origin) by PDSP assayAntagonist activity at dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 190678 0 None -2951 20 Human 5.2 pKi = 5.2 Binding
Antagonist activity at dopamine D1 receptor (unknown origin) by PDSP assayAntagonist activity at dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44436603 151994 0 None -269 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL391257 151994 0 None -269 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
11655570 86501 0 None -11220 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
CHEMBL211590 86501 0 None -11220 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
45267409 202940 0 None -1513 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL561262 202940 0 None -1513 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
71212556 150340 0 None -120 6 Human 6.2 pKi = 6.2 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 150340 0 None -120 6 Human 6.2 pKi = 6.2 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
8447 195728 84 None -8 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 195728 84 None -8 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3191 109635 97 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
145969934 171824 0 None -54 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 171824 0 None -54 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
14198573 204862 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 1 2 3.6 COc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574340 204862 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 1 2 3.6 COc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
130424 211124 14 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 327 1 1 3 4.4 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2cccc3ccoc23)C1 10.1021/jm00170a025
CHEMBL71600 211124 14 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 327 1 1 3 4.4 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2cccc3ccoc23)C1 10.1021/jm00170a025
44415827 87834 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL215414 87834 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
11619691 161835 0 None 138 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 467 3 1 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(O)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401690 161835 0 None 138 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 467 3 1 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(O)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
5311428 106883 9 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1744078 106883 9 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL287504 106883 9 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
56589560 77372 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 77372 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
1353 8692 93 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
3559 8692 93 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
86 8692 93 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
CHEMBL54 8692 93 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
DB00502 8692 93 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
6603820 102549 19 None -4 12 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.ejmech.2011.11.039
CHEMBL25856 102549 19 None -4 12 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.ejmech.2011.11.039
440229 94286 53 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 94286 53 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
6917970 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 10463 61 None -1 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
3246443 44460 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 44460 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
9869262 111638 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL310997 111638 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
3246443 44460 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 44460 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
10709445 108140 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 108140 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 108140 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10107367 109211 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 109211 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
71261649 94287 9 None 15 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334892 94287 9 None 15 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
10640108 91186 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114441 91186 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219802 91186 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
10107367 109211 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL303993 109211 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
14198585 107578 1 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 107578 1 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
10107367 109211 1 None 7 4 Human 8.2 pKi = 8.2 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL303993 109211 1 None 7 4 Human 8.2 pKi = 8.2 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
127031399 145520 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 2 6 2.8 COc1cc2c(cc1O)C1Cc3ccc(OCCCO)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780268 145520 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 2 6 2.8 COc1cc2c(cc1O)C1Cc3ccc(OCCCO)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
71109797 152674 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 152674 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
71109797 152674 0 None - 1 Human 8.2 pKi = 8.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 152674 0 None - 1 Human 8.2 pKi = 8.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
130442514 173311 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4279267 173311 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
25110709 19378 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1186967 19378 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL484538 19378 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
86764103 139215 13 None - 1 Human 8.2 pKi = 8.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697578 139215 13 None - 1 Human 8.2 pKi = 8.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415600 86560 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 461 4 1 6 4.8 COc1ccccc1CNN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL211910 86560 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 461 4 1 6 4.8 COc1ccccc1CNN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
122205437 144089 0 None -19 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 144089 0 None -19 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
12313091 93253 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1ccc2c(c1O)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2314732 93253 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1ccc2c(c1O)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
11023546 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
11023546 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
10071501 16651 0 None 10 2 Rat 7.2 pKi = 7.2 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114228 16651 0 None 10 2 Rat 7.2 pKi = 7.2 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44393415 72004 0 None -251 5 Pig 6.2 pKi = 6.2 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182652 72004 0 None -251 5 Pig 6.2 pKi = 6.2 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
137638973 163653 0 None -1479 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 163653 0 None -1479 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
56837419 76079 0 None -2630 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 76079 0 None -2630 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
46917563 75110 0 None -8511 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 75110 0 None -8511 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
2780 117306 36 None -138 10 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
CHEMBL325109 117306 36 None -138 10 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
137634153 163211 0 None -54 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 236 1 2 5 0.6 Oc1ccc(N2CCNCC2)c2c1OCCO2 10.1016/j.bmc.2017.08.037
CHEMBL4066916 163211 0 None -54 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 236 1 2 5 0.6 Oc1ccc(N2CCNCC2)c2c1OCCO2 10.1016/j.bmc.2017.08.037
10775901 42553 1 None -70 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cc(C)cc(C)c2)C1 10.1021/jm9708700
CHEMBL144114 42553 1 None -70 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cc(C)cc(C)c2)C1 10.1021/jm9708700
10609576 125530 0 None -42 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cccc(C)c2C)C1 10.1021/jm9708700
CHEMBL341825 125530 0 None -42 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cccc(C)c2C)C1 10.1021/jm9708700
72545008 99898 0 None -89 5 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 99898 0 None -89 5 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
15654859 209811 0 None 4 2 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3N(C)c3ccccc32)CC1 10.1021/jm00067a009
CHEMBL63390 209811 0 None 4 2 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3N(C)c3ccccc32)CC1 10.1021/jm00067a009
13994412 17936 1 None -117 3 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL117841 17936 1 None -117 3 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
10689791 171660 0 None 12 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 4 2 3 3.3 NCCCC(=O)N1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL422086 171660 0 None 12 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 4 2 3 3.3 NCCCC(=O)N1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
490 6979 8 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 6979 8 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 6979 8 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
10015045 20424 1 None -6 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm9015763
CHEMBL119455 20424 1 None -6 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm9015763
9992499 80161 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 80161 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
72699816 121965 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 329 3 1 4 4.1 CCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344457 121965 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 329 3 1 4 4.1 CCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
145966311 170812 0 None -3388 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cells
ChEMBL 378 5 1 4 2.9 O=C(NCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
CHEMBL4208744 170812 0 None -3388 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cells
ChEMBL 378 5 1 4 2.9 O=C(NCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
57402366 76090 0 None -1230 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 76090 0 None -1230 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
44340333 16434 0 None -1071 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 16434 0 None -1071 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340227 117418 0 None -2137 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 117418 0 None -2137 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10265732 101624 0 None 2 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253738 101624 0 None 2 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
2477 7532 59 None -28 29 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
36 7532 59 None -28 29 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
437 7532 59 None -28 29 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
CHEMBL49 7532 59 None -28 29 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
DB00490 7532 59 None -28 29 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
15508242 172028 0 None -64 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL422959 172028 0 None -64 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
838674 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL318111 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL542493 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
44316331 212278 0 None -41 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80686 212278 0 None -41 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
10378389 210024 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 210024 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 210024 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
838674 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL318111 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL542493 114202 12 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
71817345 98754 0 None -158 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
CHEMBL2414992 98754 0 None -158 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
44415567 86810 0 None 58 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212905 86810 0 None 58 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415579 86620 0 None 61 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 542 4 2 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3NC3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212186 86620 0 None 61 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 542 4 2 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3NC3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
72699817 121966 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344458 121966 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
46931072 208824 1 None -8 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 208824 1 None -8 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
2389 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 10104 118 None -489 66 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
122189391 130024 0 None -72 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 130024 0 None -72 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
44264742 103949 0 None -13 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
CHEMBL268190 103949 0 None -13 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
2 10035 23 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 10035 23 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 10035 23 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
11023546 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
9839050 119156 0 None -131 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
CHEMBL329566 119156 0 None -131 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
117773522 139222 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 6 3.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697585 139222 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 6 3.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
24863698 183477 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 253 0 2 2 2.7 Oc1ccc2c(c1)CCNCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL459871 183477 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 253 0 2 2 2.7 Oc1ccc2c(c1)CCNCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
11023546 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 85253 0 None -5 3 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
3108374 98752 24 None -3 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
CHEMBL2414990 98752 24 None -3 3 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
44400626 77177 0 None -999 5 Pig 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 77177 0 None -999 5 Pig 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
44403214 79268 0 None -446 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL198993 79268 0 None -446 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
44448063 162024 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL402736 162024 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
154727713 183143 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514586 183143 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 183143 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
118717797 121971 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 2 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344463 121971 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 2 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
10758760 29273 0 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 329 4 1 2 4.8 CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL132545 29273 0 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 329 4 1 2 4.8 CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
161379 193994 8 None -79 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
CHEMBL492418 193994 8 None -79 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
154703438 183160 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4475699 183160 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4595859 183160 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
136043857 86561 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 5.0 Clc1ccc2c(c1)N=C(N1CCN(Cc3cccc4c3OCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
CHEMBL211915 86561 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 5.0 Clc1ccc2c(c1)N=C(N1CCN(Cc3cccc4c3OCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
44281881 106625 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743774 106625 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL285717 106625 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
1242 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
44415743 86883 0 None 30 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213201 86883 0 None 30 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
6852376 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL1467585 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL24077 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL503958 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
6852376 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL1467585 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL24077 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL503958 98374 13 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
1242 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 10385 27 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
70684206 82840 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057442 82840 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692653 82841 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 82841 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
70692652 82839 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
CHEMBL2057441 82839 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
54580905 68377 0 None -2570 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 68377 0 None -2570 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
56594533 77373 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949726 77373 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
56837634 76081 0 None -1479 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 76081 0 None -1479 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
9796958 153356 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 153356 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 153356 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 153356 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
11633170 85187 0 None -2818 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
CHEMBL211118 85187 0 None -2818 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
11583188 146060 0 None -19498 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 146060 0 None -19498 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
10355510 162441 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL404865 162441 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
71461481 90845 0 None -676 5 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207632 90845 0 None -676 5 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
71450707 90853 0 None -1698 7 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 90853 0 None -1698 7 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
25131135 194327 0 None -95 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 448 6 3 5 4.7 Nc1nc2c(s1)C[C@@H](NCC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
CHEMBL494510 194327 0 None -95 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 448 6 3 5 4.7 Nc1nc2c(s1)C[C@@H](NCC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
90644058 118806 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 118806 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
90644058 118806 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 118806 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
130907 201462 5 None -3311 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm701045j
CHEMBL53294 201462 5 None -3311 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm701045j
64143 205643 62 None -1 8 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 205643 62 None -1 8 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
154725277 183211 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4472900 183211 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 183211 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
10015860 106053 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL281932 106053 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
44415598 84793 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccc(S(=O)(=O)N2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
CHEMBL209805 84793 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccc(S(=O)(=O)N2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
44415612 145733 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 6 6.0 CCOc1ccc2ccccc2c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL378512 145733 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 6 6.0 CCOc1ccc2ccccc2c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
134149077 155102 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 4 2 5 3.9 CCC(C)Oc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3936976 155102 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 4 2 5 3.9 CCC(C)Oc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
681 8247 72 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
228 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
33 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
6005 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL53 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
DB00714 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
117774495 139202 0 None - 1 Human 6.2 pKi = 6.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 396 4 1 6 2.7 Cc1cc(Oc2ncccc2N2CC(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697565 139202 0 None - 1 Human 6.2 pKi = 6.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 396 4 1 6 2.7 Cc1cc(Oc2ncccc2N2CC(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
40152769 208587 2 None -107 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL606939 208587 2 None -107 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
45481888 205793 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL585740 205793 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
21171 193755 33 None 1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL490533 193755 33 None 1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
135515431 11019 34 None -10 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
CHEMBL100454 11019 34 None -10 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
72699818 121973 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 341 3 1 4 4.1 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344466 121973 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 341 3 1 4 4.1 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
11504230 84992 0 None -870 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 84992 0 None -870 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
228 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
33 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
6005 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
CHEMBL53 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
DB00714 7233 28 None -35 23 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
44448061 101622 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253736 101622 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
45270813 203468 0 None -776 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL564709 203468 0 None -776 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
71457956 85199 0 None -87 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111527 85199 0 None -87 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
76325152 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
10037962 213486 0 None -51 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1ABinding affinity against dopamine receptor D1A
ChEMBL 254 0 1 2 3.4 c1cc2c3c(c1)c1c(n3CCNC2)CCCCCC1 10.1016/j.bmcl.2004.02.100
CHEMBL89738 213486 0 None -51 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1ABinding affinity against dopamine receptor D1A
ChEMBL 254 0 1 2 3.4 c1cc2c3c(c1)c1c(n3CCNC2)CCCCCC1 10.1016/j.bmcl.2004.02.100
118711254 120729 0 None -147 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 358 4 2 3 4.6 CN1CCc2cc(NCc3ccccc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325904 120729 0 None -147 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 358 4 2 3 4.6 CN1CCc2cc(NCc3ccccc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
42626315 63024 0 None -1445 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627320 63024 0 None -1445 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
10363751 169859 0 None -1584 3 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 402 6 0 4 3.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(F)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL417661 169859 0 None -1584 3 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 402 6 0 4 3.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(F)cc2)C1 10.1016/s0960-894x(99)00201-2
45269974 20394 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194307 20394 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550792 20394 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
91899756 136217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cc(=O)[nH]nc1C nan
CHEMBL3671295 136217 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cc(=O)[nH]nc1C nan
9888555 172383 16 None -3235 8 Human 6.2 pKi = 6.2 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 172383 16 None -3235 8 Human 6.2 pKi = 6.2 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
25071691 118564 0 None -2818 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 118564 0 None -2818 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
6469918 86666 13 None -954 6 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 86666 13 None -954 6 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
71450812 85197 0 None -338 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111525 85197 0 None -338 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
3036864 209533 19 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 209533 19 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 209533 19 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 209533 19 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
10360174 175027 1 None -2 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 344 0 0 5 3.5 CN1CCN(C2=Nc3cccnc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL433744 175027 1 None -2 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 344 0 0 5 3.5 CN1CCN(C2=Nc3cccnc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
10660476 54147 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
CHEMBL154468 54147 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
15654856 209803 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 311 0 1 5 2.6 CN1CCN(C2=Nc3cccnc3Nc3ccc(F)cc32)CC1 10.1021/jm00067a009
CHEMBL63347 209803 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 311 0 1 5 2.6 CN1CCN(C2=Nc3cccnc3Nc3ccc(F)cc32)CC1 10.1021/jm00067a009
42625207 63008 0 None -257 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627304 63008 0 None -257 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
44323890 213696 0 None 1 4 Rat 7.2 pKi = 7.2 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90977 213696 0 None 1 4 Rat 7.2 pKi = 7.2 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
3039881 181036 10 None 4 3 Human 7.2 pKi = 7.2 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 181036 10 None 4 3 Human 7.2 pKi = 7.2 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
44415638 86659 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212334 86659 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415490 146016 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378886 146016 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134150645 158424 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 475 7 2 5 5.5 CCCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3963862 158424 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 475 7 2 5 5.5 CCCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
44300069 202896 0 None 35 2 Rat 7.2 pKi = 7.2 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56100 202896 0 None 35 2 Rat 7.2 pKi = 7.2 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
41532205 85052 1 None -954 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210717 85052 1 None -954 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
11504230 84992 0 None -1023 7 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
CHEMBL210567 84992 0 None -1023 7 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
145990141 173558 0 None -323 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283982 173558 0 None -323 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
44454709 104294 0 None -5248 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL270406 104294 0 None -5248 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
12888943 16341 0 None -812 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL112395 16341 0 None -812 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
10660476 54147 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
CHEMBL154468 54147 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
25139332 191098 0 None -7 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL484204 191098 0 None -7 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
16121920 202654 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL558838 202654 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
45267435 202770 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
CHEMBL559868 202770 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
52937776 67944 0 None -9549 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765629 67944 0 None -9549 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
127046948 146848 0 None -295 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 146848 0 None -295 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
118709168 120192 0 None -33 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318840 120192 0 None -33 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12050200 108867 0 None -128 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL302186 108867 0 None -128 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
11708363 78677 1 None -23 4 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL197159 78677 1 None -23 4 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
44329057 214774 0 None -93 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97283 214774 0 None -93 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
86767109 136224 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 6 3.5 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
CHEMBL3671301 136224 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 6 3.5 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
52940985 24358 0 None -69 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258155 24358 0 None -69 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
10666053 107162 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289927 107162 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
156013324 184272 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 310 2 1 4 3.0 COc1cc2c3c(c1OC)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4639398 184272 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 310 2 1 4 3.0 COc1cc2c3c(c1OC)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
76325152 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 113148 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
90140337 136192 0 None - 1 Human 6.2 pKi = 6.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 4 2 6 3.1 COc1cnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c2c[nH]nc12 nan
CHEMBL3671271 136192 0 None - 1 Human 6.2 pKi = 6.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 4 2 6 3.1 COc1cnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c2c[nH]nc12 nan
10333842 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL27559 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
10333842 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.06.016
CHEMBL27559 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.06.016
10333842 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.11.025
CHEMBL27559 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.11.025
681 8247 72 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
14371639 109900 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00170a025
CHEMBL307790 109900 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00170a025
46231646 207244 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL598515 207244 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
14371639 109900 0 None - 1 Human 8.2 pKi = 8.2 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00081a010
CHEMBL307790 109900 0 None - 1 Human 8.2 pKi = 8.2 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00081a010
44415826 87166 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL214503 87166 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415705 145444 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 2 2 6 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL377756 145444 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 2 2 6 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
1218 10388 30 None -11 8 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
938 10388 30 None -11 8 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL353335 10388 30 None -11 8 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
11306892 208085 0 None 79 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)Nc4c(Cl)cccc4Cl)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL604129 208085 0 None 79 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)Nc4c(Cl)cccc4Cl)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
15069446 205490 0 None 213 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 293 0 1 2 3.6 Cc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL58205 205490 0 None 213 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 293 0 1 2 3.6 Cc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
44415594 87034 0 None 177 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213882 87034 0 None 177 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
135398737 7745 93 None -44 90 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
38 7745 93 None -44 90 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
722 7745 93 None -44 90 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
CHEMBL42 7745 93 None -44 90 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
DB00363 7745 93 None -44 90 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
71109804 94281 0 None 12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 10.1016/j.bmc.2012.12.016
CHEMBL2334882 94281 0 None 12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 10.1016/j.bmc.2012.12.016
71109805 94280 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
CHEMBL2334881 94280 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
15937727 123356 0 None 158 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 307 1 1 2 4.6 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL336532 123356 0 None 158 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 307 1 1 2 4.6 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCCC2)C1 10.1016/S0960-894X(00)80155-9
11536995 146333 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 146333 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
86764210 139216 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 1 4 4.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697579 139216 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 1 4 4.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
44415552 87015 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
CHEMBL213795 87015 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
134157446 160565 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 371 5 2 6 2.8 COCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3982215 160565 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 371 5 2 6 2.8 COCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
9901453 135266 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 315 1 0 4 3.3 CN1CCN(C2=Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm0309811
CHEMBL366679 135266 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 315 1 0 4 3.3 CN1CCN(C2=Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm0309811
44415595 86668 0 None 27 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 3 1 6 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212383 86668 0 None 27 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 3 1 6 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
127031423 145540 0 None 6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 369 5 1 5 3.9 CCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3780506 145540 0 None 6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 369 5 1 5 3.9 CCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
162672733 189798 0 None 102 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 317 1 1 3 4.8 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4793813 189798 0 None 102 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 317 1 1 3 4.8 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
44316024 212232 0 None -2 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 249 5 2 3 2.9 CCCCN1CCCC1Cc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL80369 212232 0 None -2 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 249 5 2 3 2.9 CCCCN1CCCC1Cc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
70690498 82842 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 82842 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
74223774 136203 0 None - 1 Human 8.1 pKi = 8.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 5 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc2nccn12 nan
CHEMBL3671282 136203 0 None - 1 Human 8.1 pKi = 8.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 5 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc2nccn12 nan
17756213 156483 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 156483 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
135398745 9688 112 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 9688 112 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 9688 112 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 9688 112 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
10540201 107005 0 None 4 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL288536 107005 0 None 4 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
1353 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
3559 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
86 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
CHEMBL54 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
DB00502 8692 93 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
10333842 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL27559 105207 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
13678336 208761 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 289 1 3 3 3.1 Oc1c(O)c(-c2ccccc2)c2c(c1Cl)CCNCC2 10.1021/jm00160a018
CHEMBL60808 208761 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 289 1 3 3 3.1 Oc1c(O)c(-c2ccccc2)c2c(c1Cl)CCNCC2 10.1021/jm00160a018
10610641 105695 0 None -47 5 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 249 0 0 1 3.7 Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL27940 105695 0 None -47 5 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 249 0 0 1 3.7 Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
11638780 83870 0 None -1737 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL207488 83870 0 None -1737 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
70686495 83344 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccc(Br)cc3)[C@H]21 10.1016/j.ejmech.2012.07.025
CHEMBL2062856 83344 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccc(Br)cc3)[C@H]21 10.1016/j.ejmech.2012.07.025
44372198 55914 0 None -239 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL156198 55914 0 None -239 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
44270444 56098 0 None -138 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL156369 56098 0 None -138 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
11078813 118795 0 None -19 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL328925 118795 0 None -19 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
12928483 20119 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
CHEMBL1192258 20119 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
CHEMBL543472 20119 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
44320116 170887 0 None 7 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 170887 0 None 7 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
10810641 16164 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL111509 16164 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL544089 16164 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
156011233 184078 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 334 3 1 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636589 184078 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 334 3 1 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
44415599 145229 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccccc1S(=O)(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL377452 145229 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccccc1S(=O)(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
9857902 67578 0 None -26 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
CHEMBL176169 67578 0 None -26 4 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
15115512 16169 7 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 324 6 2 3 3.8 CCCN(CCc1ccc(N)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL111532 16169 7 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 324 6 2 3 3.8 CCCN(CCc1ccc(N)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
25093832 162659 0 None -2290 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 162659 0 None -2290 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
11574902 85225 0 None -28183 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
CHEMBL211164 85225 0 None -28183 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
44339953 116477 0 None -707 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 116477 0 None -707 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
17469721 84800 5 None -22 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL209832 84800 5 None -22 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
45271691 202332 0 None -107 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL554692 202332 0 None -107 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44372338 60620 0 None -2511 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160454 60620 0 None -2511 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44329099 214860 0 None -40 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97750 214860 0 None -40 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
25186023 194523 0 None -50118 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl 10.1021/jm800689g
CHEMBL495572 194523 0 None -50118 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl 10.1021/jm800689g
10527469 163044 3 None -1548 16 Mouse 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 163044 3 None -1548 16 Mouse 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
10421583 105959 1 None -9 5 Rat 6.1 pKi = 6.1 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 235 0 0 1 3.4 CN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm960189i
CHEMBL281357 105959 1 None -9 5 Rat 6.1 pKi = 6.1 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 235 0 0 1 3.4 CN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm960189i
CHEMBL4520788 220754 10 None -33 25 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a DRD1
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
72699904 121977 0 None -60 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 377 5 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344470 121977 0 None -60 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 377 5 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
44385715 67849 0 None 1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 280 1 0 2 3.8 CN1CCc2cccc3c2c(cn3-c2ccc(F)cc2)C1 10.1016/s0960-894x(98)00138-3
CHEMBL176476 67849 0 None 1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 280 1 0 2 3.8 CN1CCc2cccc3c2c(cn3-c2ccc(F)cc2)C1 10.1016/s0960-894x(98)00138-3
156011458 184083 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4636741 184083 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
228 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
33 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
6005 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
CHEMBL53 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
DB00714 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
228 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
33 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
6005 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
CHEMBL53 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
DB00714 7233 28 None -35 23 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
13869641 120180 0 None -29 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318824 120180 0 None -29 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9819674 19706 0 None -10 4 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL118919 19706 0 None -10 4 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
74223827 136220 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 335 3 1 5 4.0 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
CHEMBL3671298 136220 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 335 3 1 5 4.0 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
9819674 19706 0 None -10 4 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL118919 19706 0 None -10 4 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
11208237 107751 0 None 109 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 279 0 1 2 3.3 CN1CCc2ccc(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL294221 107751 0 None 109 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 279 0 1 2 3.3 CN1CCc2ccc(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
10849018 20709 0 None -120 3 Rat 6.1 pKi = 6.1 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 261 1 0 1 4.1 C=Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL119656 20709 0 None -120 3 Rat 6.1 pKi = 6.1 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 261 1 0 1 4.1 C=Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
44400585 75430 0 None -1949 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 75430 0 None -1949 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10425969 107785 3 None -1862 4 Bovine 5.1 pKi = 5.1 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294459 107785 3 None -1862 4 Bovine 5.1 pKi = 5.1 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
14809026 212566 3 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL83080 212566 3 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
14809026 212566 3 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL83080 212566 3 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
10551026 108394 0 None -724 5 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 108394 0 None -724 5 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44448067 162308 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
CHEMBL404240 162308 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
2 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
54562 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
CHEMBL240773 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
12050194 209670 1 None -50 4 Bovine 4.1 pKi = 4.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL62703 209670 1 None -50 4 Bovine 4.1 pKi = 4.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
133633 9021 53 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 9021 53 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 9021 53 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
10378389 210024 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 210024 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 210024 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
156020120 184812 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 340 3 0 5 3.4 COc1cc2c3c(c1OC)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4646927 184812 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 340 3 0 5 3.4 COc1cc2c3c(c1OC)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
15654860 210440 1 None 2 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ncccc32)CC1 10.1021/jm00067a009
CHEMBL67355 210440 1 None 2 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ncccc32)CC1 10.1021/jm00067a009
45481840 204838 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 267 4 0 2 4.1 CCCCC1c2cc(OC)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
CHEMBL574110 204838 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 267 4 0 2 4.1 CCCCC1c2cc(OC)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
6852376 98374 13 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL1467585 98374 13 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL24077 98374 13 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL503958 98374 13 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
10588326 165645 0 None 17 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL40950 165645 0 None 17 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
44436608 153534 0 None -870 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 153534 0 None -870 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
167715 9651 14 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
969 9651 14 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
CHEMBL225230 9651 14 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
3033276 19949 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
CHEMBL1190928 19949 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
CHEMBL541867 19949 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
25139331 176707 0 None -1 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL444128 176707 0 None -1 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
24823920 104222 0 None -26 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
CHEMBL270056 104222 0 None -26 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
53325137 65368 0 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684128 65368 0 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
10324985 83556 8 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 83556 8 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 83556 8 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
14659294 174768 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 301 0 2 3 3.5 CN1CCc2cc(Cl)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL431946 174768 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 301 0 2 3 3.5 CN1CCc2cc(Cl)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
70692653 82841 0 None - 1 Human 7.1 pKi = 7.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 82841 0 None - 1 Human 7.1 pKi = 7.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
70692653 82841 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057443 82841 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
129012255 161157 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)C1Cc3c(c(OC)cc(OC)c3OC)CN1CC2 nan
CHEMBL3987156 161157 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)C1Cc3c(c(OC)cc(OC)c3OC)CN1CC2 nan
71454295 90854 0 None -933 7 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 90854 0 None -933 7 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
57398875 76089 0 None -213 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 76089 0 None -213 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
71474024 151246 0 None - 1 Human 6.1 pKi = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3906676 151246 0 None - 1 Human 6.1 pKi = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
10551026 108394 0 None -724 5 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 108394 0 None -724 5 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
15691846 211438 0 None -10 2 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 335 3 1 3 3.4 O=C1CC(CN2CCC(O)(c3ccccc3)CC2)Cc2ccccc21 10.1021/jm00111a046
CHEMBL73675 211438 0 None -10 2 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 335 3 1 3 3.4 O=C1CC(CN2CCC(O)(c3ccccc3)CC2)Cc2ccccc21 10.1021/jm00111a046
10672006 53593 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 467 5 1 3 5.5 CCCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
CHEMBL154015 53593 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 467 5 1 3 5.5 CCCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
14198588 178286 2 None 2 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 178286 2 None 2 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
14198589 69848 2 None 35 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@@H]2c1ccccc1 10.1021/jm00118a012
CHEMBL1788322 69848 2 None 35 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@@H]2c1ccccc1 10.1021/jm00118a012
9928332 103955 5 None -371 9 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assayCompound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
CHEMBL268258 103955 5 None -371 9 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assayCompound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
2585 7590 103 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
10665177 29915 0 None 56 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 344 5 2 3 3.8 NCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL133094 29915 0 None 56 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 344 5 2 3 3.8 NCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10620219 13790 0 None 46 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 386 8 2 3 4.8 CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL108480 13790 0 None 46 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 386 8 2 3 4.8 CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
1353 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
3559 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
86 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
CHEMBL54 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
DB00502 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
45482152 204789 0 None -131 4 Pig 6.1 pKi = 6.1 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
CHEMBL573792 204789 0 None -131 4 Pig 6.1 pKi = 6.1 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
4420454 63033 6 None -41 5 Bovine 6.1 pKi = 6.1 Binding
Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None -41 5 Bovine 6.1 pKi = 6.1 Binding
Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44400500 172839 0 None -380 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL425731 172839 0 None -380 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10980338 174787 0 None -2454 4 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
CHEMBL432059 174787 0 None -2454 4 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
10498094 39092 1 None -5370 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
CHEMBL141035 39092 1 None -5370 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
44412494 85096 0 None -2630 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210955 85096 0 None -2630 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
137643132 164829 0 None -6309 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 164829 0 None -6309 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
44381146 65281 0 None -18 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168372 65281 0 None -18 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
11639064 196721 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL458579 196721 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL517028 196721 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
156012686 184141 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 352 3 1 4 3.4 COc1cc2c3c(c1OC)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4637673 184141 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 352 3 1 4 3.4 COc1cc2c3c(c1OC)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
118711258 120733 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)cc1 10.1016/j.ejmech.2014.07.059
CHEMBL3325908 120733 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)cc1 10.1016/j.ejmech.2014.07.059
10040938 51134 0 None 1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 308 0 0 5 2.8 Cc1ccc2c(c1)N=C(N1CCN(C)CC1)c1cccnc1O2 10.1021/jm00030a011
CHEMBL151809 51134 0 None 1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 308 0 0 5 2.8 Cc1ccc2c(c1)N=C(N1CCN(C)CC1)c1cccnc1O2 10.1021/jm00030a011
10044041 55717 0 None -8 2 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 359 1 0 3 4.3 COc1ccc2c(c1)CC1c3c(ccc(Br)c3CCN1C)O2 10.1021/jm991034o
CHEMBL156011 55717 0 None -8 2 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 359 1 0 3 4.3 COc1ccc2c(c1)CC1c3c(ccc(Br)c3CCN1C)O2 10.1021/jm991034o
1353 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
3559 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
86 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
CHEMBL54 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
DB00502 8692 93 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
156015018 184350 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4640497 184350 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
129103318 174093 0 None -107 13 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 174093 0 None -107 13 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
3038495 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
3038495 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 7495 37 None -616 18 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
3038495 7495 37 None -512 18 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 7495 37 None -512 18 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 7495 37 None -512 18 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
44263882 104000 0 None -4 3 Bovine 5.1 pKi = 5.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268558 104000 0 None -4 3 Bovine 5.1 pKi = 5.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
25333445 84898 5 None -380 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210318 84898 5 None -380 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44567596 196562 0 None -12 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 371 6 3 6 2.2 CN1CCc2cc(OCCOCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL516151 196562 0 None -12 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 371 6 3 6 2.2 CN1CCc2cc(OCCOCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
126720252 171454 0 None -269 12 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 171454 0 None -269 12 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
11222444 136962 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 369 4 0 5 4.1 CC(C)OCc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
CHEMBL367875 136962 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 369 4 0 5 4.1 CC(C)OCc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
10873978 175265 0 None -18 5 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL435218 175265 0 None -18 5 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
117774120 139230 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 6 3.3 COC(=O)c1cccnc1Oc1ccc(-c2c(C)n[nH]c(=O)c2C)c(C)c1 nan
CHEMBL3697592 139230 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 6 3.3 COC(=O)c1cccnc1Oc1ccc(-c2c(C)n[nH]c(=O)c2C)c(C)c1 nan
26987 7736 33 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 7736 33 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 7736 33 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 7736 33 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 7736 33 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
11631304 80151 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
CHEMBL201432 80151 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
71817345 98754 0 None -158 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
CHEMBL2414992 98754 0 None -158 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
1588 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
28864 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
43 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
CHEMBL157138 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
DB00589 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
117949705 121975 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344468 121975 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
134150400 158759 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 397 7 2 5 4.7 CCCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3966718 158759 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 397 7 2 5 4.7 CCCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
44436618 154701 0 None -512 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL393365 154701 0 None -512 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
11581237 145736 0 None -4897 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
CHEMBL378515 145736 0 None -4897 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
137637428 163015 0 None -9 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4064759 163015 0 None -9 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
72545010 99900 0 None -229 5 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 99900 0 None -229 5 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
11091738 124870 0 None -22 5 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
CHEMBL340641 124870 0 None -22 5 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
11102533 24829 0 None -13 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 457 8 1 6 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2nc3ccccc3n3cccc23)CC1 10.1021/jm0211220
CHEMBL126590 24829 0 None -13 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 457 8 1 6 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2nc3ccccc3n3cccc23)CC1 10.1021/jm0211220
2274 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44568533 195623 0 None 8 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 280 1 1 3 3.0 COc1cc2c3c(c1)-c1c(N)cccc1C[C@H]3N(C)CC2 10.1016/j.bmc.2008.05.077
CHEMBL506721 195623 0 None 8 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 280 1 1 3 3.0 COc1cc2c3c(c1)-c1c(N)cccc1C[C@H]3N(C)CC2 10.1016/j.bmc.2008.05.077
10758744 107283 0 None 11 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL291100 107283 0 None 11 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
162653702 187283 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4753299 187283 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
11699469 84427 0 None -48 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
CHEMBL208847 84427 0 None -48 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
49783041 23943 0 None -1949 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256171 23943 0 None -1949 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
10826543 16873 0 None -85 3 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 1 2 3.7 CCc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL115524 16873 0 None -85 3 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 1 2 3.7 CCc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
277 8083 62 None -33 50 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 8083 62 None -33 50 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 8083 62 None -33 50 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 8083 62 None -33 50 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 8083 62 None -33 50 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
44415382 87882 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 4 1 5 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL215611 87882 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 4 1 5 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
44241718 202043 0 None -281 4 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL551199 202043 0 None -281 4 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10709445 108140 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 108140 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 108140 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
90644064 118813 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289649 118813 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
154724609 183378 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514800 183378 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 183378 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
53325242 63844 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 63844 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
15981509 148736 1 None 316 2 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 148736 1 None 316 2 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
130907 201462 5 None -7 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
CHEMBL53294 201462 5 None -7 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
10448562 121898 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 121898 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
9995986 35042 1 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL137420 35042 1 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
10448562 121898 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 121898 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
117773687 139207 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.6 C=C(C)c1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697570 139207 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.6 C=C(C)c1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
130442534 173676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286177 173676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
10851849 176712 0 None 16 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL44414 176712 0 None 16 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
13372 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
86764100 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
CHEMBL3697617 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
DB14899 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C nan
13372 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 10.1021/acs.jmedchem.8b01767
86764100 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 10.1021/acs.jmedchem.8b01767
CHEMBL3697617 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 10.1021/acs.jmedchem.8b01767
DB14899 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 10.1021/acs.jmedchem.8b01767
9818423 115026 0 None 34 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 281 0 3 3 3.0 Cc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
CHEMBL319707 115026 0 None 34 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 281 0 3 3 3.0 Cc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
15937719 25584 0 None 72 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 249 1 1 2 2.6 C#CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL127843 25584 0 None 72 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 249 1 1 2 2.6 C#CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
11522339 82027 1 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 82027 1 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
173871 10386 2 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
936 10386 2 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
CHEMBL1193571 10386 2 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
75201901 173204 19 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 173204 19 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
11716438 147660 1 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 147660 1 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
163091 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
22 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
CHEMBL504548 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
6603797 74793 4 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL1257041 74793 4 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL19130 74793 4 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
44447997 102517 0 None -20 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 4 0 3 3.9 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1cccc(OC=O)c1-3 10.1021/jm060959i
CHEMBL258372 102517 0 None -20 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 4 0 3 3.9 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1cccc(OC=O)c1-3 10.1021/jm060959i
9888555 172383 16 None -3235 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 172383 16 None -3235 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
137651936 164171 0 None -1000 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 164171 0 None -1000 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
145990453 173724 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287062 173724 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
145993377 173747 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287471 173747 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
70690652 83345 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccc(Br)cc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
CHEMBL2062857 83345 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccc(Br)cc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
12050202 210077 0 None -204 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64752 210077 0 None -204 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44329067 214785 0 None -154 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2ccc(C=O)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97319 214785 0 None -154 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2ccc(C=O)c2C1 10.1016/s0960-894x(01)00564-9
1240 15595 17 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109684 15595 17 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL1256754 15595 17 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
44415758 86821 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 521 4 1 5 6.1 CC(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212950 86821 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 521 4 1 5 6.1 CC(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
57391896 76080 0 None -125 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 76080 0 None -125 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
10758745 107209 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 107209 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 107209 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10427977 61239 0 None -660 4 Bovine 6.1 pKi = 6.1 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160952 61239 0 None -660 4 Bovine 6.1 pKi = 6.1 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
57395341 76086 0 None -426 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 76086 0 None -426 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
9842468 16681 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL114375 16681 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
9842468 16681 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL114375 16681 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10088453 72849 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1016/j.bmcl.2004.06.005
CHEMBL183776 72849 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1016/j.bmcl.2004.06.005
10088453 72849 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1007/s00044-012-0055-5
CHEMBL183776 72849 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1007/s00044-012-0055-5
9972693 175304 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cccnc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL435441 175304 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cccnc3Sc3ccccc32)CC1 10.1021/jm00030a011
76321554 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
14198577 204895 0 None 2 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 0 2 3.9 COc1cc2c(cc1Cl)CCN(C)C2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574557 204895 0 None 2 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 0 2 3.9 COc1cc2c(cc1Cl)CCN(C)C2c1ccccc1 10.1016/j.bmc.2009.05.079
154726353 183102 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4577162 183102 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 183102 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1353 8692 93 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 8692 93 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 8692 93 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 8692 93 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 8692 93 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
11500677 147626 1 None -6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 147626 1 None -6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
117773662 139217 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 3.7 CCc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)n(C)c(=O)[nH]c1=O nan
CHEMBL3697580 139217 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 3.7 CCc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)n(C)c(=O)[nH]c1=O nan
86764101 139255 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
CHEMBL3697618 139255 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
117773616 139192 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.1 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697555 139192 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.1 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
117773980 139210 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 2 6 2.3 Cc1cc(Oc2ncccc2O)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697573 139210 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 2 6 2.3 Cc1cc(Oc2ncccc2O)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44393393 130451 0 None -575 5 Pig 6.1 pKi = 6.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
CHEMBL362101 130451 0 None -575 5 Pig 6.1 pKi = 6.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
9888555 172383 16 None -3548 8 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
CHEMBL424294 172383 16 None -3548 8 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
44340084 15860 0 None -2238 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 15860 0 None -2238 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
56597938 10712 3 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 10712 3 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 10712 3 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
117772974 139206 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 414 4 1 6 3.0 Cc1cc(Oc2ncccc2N2CC(F)(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697569 139206 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 414 4 1 6 3.0 Cc1cc(Oc2ncccc2N2CC(F)(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415648 86945 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213472 86945 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
17755868 149896 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 149896 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44401243 175273 0 None -34 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL435301 175273 0 None -34 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
156022132 184996 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 4 1 4 3.6 C=CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4649785 184996 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 4 1 4 3.6 C=CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
10085358 116996 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
CHEMBL323771 116996 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
44448064 101649 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253947 101649 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
44264641 211581 1 None -11 3 Bovine 4.1 pKi = 4.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7505 211581 1 None -11 3 Bovine 4.1 pKi = 4.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
44329293 116845 0 None -75 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL323557 116845 0 None -75 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
145968810 171817 0 None -120 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 171817 0 None -120 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
154725813 183305 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4568916 183305 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 183305 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
127031404 145580 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 4 2 5 3.2 COc1cc2c(cc1O)C(C)N(Cc1cccc(O)c1OC)CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780975 145580 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 4 2 5 3.2 COc1cc2c(cc1O)C(C)N(Cc1cccc(O)c1OC)CC2 10.1016/j.bmc.2016.03.037
136043856 86882 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 438 2 1 4 5.6 Fc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(F)c1 10.1016/j.bmcl.2006.06.034
CHEMBL213200 86882 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 438 2 1 4 5.6 Fc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(F)c1 10.1016/j.bmcl.2006.06.034
71062708 161085 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 161085 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
90644060 118808 0 None -64 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
CHEMBL3289644 118808 0 None -64 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
103 10925 61 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 10925 61 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 10925 61 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 10925 61 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 10925 61 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
1248739 146864 16 None -190 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL380054 146864 16 None -190 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
44339984 174576 0 None -186 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 174576 0 None -186 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
135524323 202205 0 None -3467 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
CHEMBL552268 202205 0 None -3467 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
45272537 203305 0 None -588 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563614 203305 0 None -588 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
44415804 88250 0 None 147 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL215997 88250 0 None 147 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
135398745 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
47 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
CHEMBL715 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
DB00334 9688 112 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
15627811 201711 1 None -8 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL54183 201711 1 None -8 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
44405980 78831 0 None -23 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
CHEMBL197656 78831 0 None -23 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
1588 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None -131 44 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
44415606 86891 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
CHEMBL213239 86891 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
44415823 148235 0 None 331 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccncc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL384248 148235 0 None 331 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccncc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415473 86697 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 437 1 1 5 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212486 86697 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 437 1 1 5 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
118709177 120202 0 None -16 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318850 120202 0 None -16 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
86764213 139228 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 1 5 4.2 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697590 139228 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 1 5 4.2 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
15711850 20011 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1191350 20011 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL542436 20011 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
117949627 121934 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 287 1 1 4 3.1 COc1cc2c(cc1O)[C@@H]1Cc3sccc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344356 121934 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 287 1 1 4 3.1 COc1cc2c(cc1O)[C@@H]1Cc3sccc3CN1CC2 10.1016/j.bmc.2014.09.024
44436621 97806 0 None -151 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL239733 97806 0 None -151 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
71456045 90848 0 None -1202 6 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 90848 0 None -1202 6 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
127046952 146879 0 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 146879 0 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
25093832 162659 0 None -2290 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 162659 0 None -2290 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137640391 163484 0 None -1096 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 163484 0 None -1096 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137635364 163039 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 163039 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4074669 163039 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
10314824 42154 1 None -8511 5 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 42154 1 None -8511 5 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
10314824 42154 1 None -8511 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL143761 42154 1 None -8511 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
44448060 162023 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
CHEMBL402735 162023 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
137657153 166336 0 None -776 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 166336 0 None -776 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
85658088 171782 0 None -2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 171782 0 None -2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
1043 8363 14 None -9549 29 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -9549 29 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -9549 29 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -9549 29 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -9549 29 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
135986088 184894 0 None -263 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
CHEMBL464811 184894 0 None -263 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
76321554 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 113180 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
112500029 139244 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 0 6 3.9 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697606 139244 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 0 6 3.9 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)ncc(=O)n1C nan
14198596 108420 0 None 2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 108420 0 None 2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
14198597 108901 1 None 3 2 Human 7.1 pKi = 7.1 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL302393 108901 1 None 3 2 Human 7.1 pKi = 7.1 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00129a006
117772840 139214 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 343 3 1 5 2.9 Cc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697577 139214 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 343 3 1 5 2.9 Cc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
44320129 174673 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL431220 174673 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
16105548 89473 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL217964 89473 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL221652 89473 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
53363200 70627 0 None -134 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803052 70627 0 None -134 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
11682812 84984 0 None -5495 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
CHEMBL210551 84984 0 None -5495 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
2 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 10035 23 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44380716 65861 0 None -12 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL169631 65861 0 None -12 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
2 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
54562 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
CHEMBL240773 10035 23 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
2 10035 23 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 10035 23 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 10035 23 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
44582179 188204 0 None -57 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 379 6 0 5 2.5 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476393 188204 0 None -57 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 379 6 0 5 2.5 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2009.01.067
154706431 183364 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4531363 183364 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 183364 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
1220 6975 55 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
31 6975 55 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
7 6975 55 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
CHEMBL56 6975 55 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
44591012 182359 0 None -177 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL457957 182359 0 None -177 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
44386883 67174 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 328 3 1 4 3.2 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CNCC2 10.1016/s0960-894x(98)00138-3
CHEMBL174949 67174 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 328 3 1 4 3.2 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CNCC2 10.1016/s0960-894x(98)00138-3
44415845 86788 0 None 34 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 511 3 1 7 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3-n3ccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212844 86788 0 None 34 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 511 3 1 7 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3-n3ccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11515697 185011 0 None -7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL458397 185011 0 None -7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL465054 185011 0 None -7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
86767093 136201 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
CHEMBL3671280 136201 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
10574176 16734 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 420 5 1 3 5.3 CN(C)c1ccc(CCN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114726 16734 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 420 5 1 3 5.3 CN(C)c1ccc(CCN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44320026 212878 0 None 3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85689 212878 0 None 3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
117774323 139198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.9 Cc1cc(Oc2ncc(Cl)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697561 139198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.9 Cc1cc(Oc2ncc(Cl)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
10643780 126173 0 None -97 4 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL344602 126173 0 None -97 4 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
10276451 207064 37 None -3388 9 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL2112910 207064 37 None -3388 9 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL59725 207064 37 None -3388 9 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
10276451 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL2112910 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL59725 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
10276451 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL2112910 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL59725 207064 37 None -9120 9 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
137632607 163118 0 None -2344 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4065797 163118 0 None -2344 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
44278298 105940 0 None -2884 3 Rat 4.1 pKi = 4.1 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 348 4 0 2 4.3 O=C(c1cccc(CN2CCC(c3ccccc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
CHEMBL281214 105940 0 None -2884 3 Rat 4.1 pKi = 4.1 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 348 4 0 2 4.3 O=C(c1cccc(CN2CCC(c3ccccc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
44304652 207101 0 None -28 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 207101 0 None -28 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
44415622 145381 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 591 4 1 5 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc(F)cc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL377564 145381 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 591 4 1 5 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc(F)cc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
228 7233 28 None -30 23 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
33 7233 28 None -30 23 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
6005 7233 28 None -30 23 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
CHEMBL53 7233 28 None -30 23 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
DB00714 7233 28 None -30 23 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
180 7189 56 None -109 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
200 7189 56 None -109 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
2160 7189 56 None -109 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL629 7189 56 None -109 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
DB00321 7189 56 None -109 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
135398737 7745 93 None -44 90 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
38 7745 93 None -44 90 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
722 7745 93 None -44 90 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL42 7745 93 None -44 90 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
DB00363 7745 93 None -44 90 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
44276652 106270 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL283247 106270 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
127045855 146442 0 None -9 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 146442 0 None -9 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
44381276 65502 0 None -2 4 Bovine 5.1 pKi = 5.1 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168541 65502 0 None -2 4 Bovine 5.1 pKi = 5.1 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44304644 210030 0 None -8 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
CHEMBL64566 210030 0 None -8 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
154703922 183068 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4590211 183068 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 183068 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
154703824 183405 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4456007 183405 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 183405 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
181743 185351 5 None -446 22 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH233930 from human dopamine D1 receptorDisplacement of [3H]SCH233930 from human dopamine D1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 185351 5 None -446 22 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH233930 from human dopamine D1 receptorDisplacement of [3H]SCH233930 from human dopamine D1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
242 7258 124 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 7258 124 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 7258 124 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 7258 124 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 7258 124 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
44304621 210198 0 None -74 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL65641 210198 0 None -74 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
6101909 107713 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
CHEMBL294012 107713 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
6101909 107713 1 None -1 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
CHEMBL294012 107713 1 None -1 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
44455426 161928 0 None -12 12 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 161928 0 None -12 12 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44415629 86805 0 None 338 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccsc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212896 86805 0 None 338 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccsc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
10107367 109211 1 None -7 4 Rat 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 109211 1 None -7 4 Rat 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
44385980 68158 0 None 3 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 268 1 1 2 3.2 Fc1ccc(N2CC3CNCCc4cccc2c43)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL176990 68158 0 None 3 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 268 1 1 2 3.2 Fc1ccc(N2CC3CNCCc4cccc2c43)cc1 10.1016/s0960-894x(98)00138-3
11558247 82197 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 82197 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
86764211 139224 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697587 139224 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
11573806 82191 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 82191 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
2865 10915 73 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 10915 73 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 10915 73 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 10915 73 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 10915 73 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
1353 8692 93 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
3559 8692 93 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
86 8692 93 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
CHEMBL54 8692 93 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
DB00502 8692 93 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
10830233 209632 0 None 8 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 329 0 2 1 4.3 CN1CCc2c([nH]c3ccccc23)Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
CHEMBL62529 209632 0 None 8 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 329 0 2 1 4.3 CN1CCc2c([nH]c3ccccc23)Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
117774170 139213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 385 3 1 4 4.3 Cc1cc(Oc2ncccc2Br)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697576 139213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 385 3 1 4 4.3 Cc1cc(Oc2ncccc2Br)ccc1-c1c(C)n[nH]c(=O)c1C nan
134137323 149745 0 None 33 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 4 2 5 4.7 CCC(C)Oc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3894329 149745 0 None 33 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 4 2 5 4.7 CCC(C)Oc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
74223724 136195 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671274 136195 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223777 136213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 350 3 1 4 5.1 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1Cl nan
CHEMBL3671291 136213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 350 3 1 4 5.1 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1Cl nan
44393403 71852 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 71852 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
137655735 165771 0 None -1230 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 165771 0 None -1230 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
52943802 24390 0 None -199 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258270 24390 0 None -199 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
44319368 112841 0 None -7 4 Bovine 5.1 pKi = 5.1 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 112841 0 None -7 4 Bovine 5.1 pKi = 5.1 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
10807793 209758 1 None 7 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 350 2 1 3 3.8 COc1cc2c(cc1OC)Cc1[nH]c3ccccc3c1CCN(C)CC2 10.1021/jm9911478
CHEMBL63063 209758 1 None 7 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 350 2 1 3 3.8 COc1cc2c(cc1OC)Cc1[nH]c3ccccc3c1CCN(C)CC2 10.1021/jm9911478
164627027 193206 0 None -45 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
CHEMBL4876260 193206 0 None -45 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
44403224 78690 0 None -102 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
CHEMBL197195 78690 0 None -102 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
44436605 155842 0 None -2951 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 155842 0 None -2951 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
53318564 65369 0 None -8 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 646 14 0 7 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCN(CCCN2CCN(c4ccccc4OC)CC2)S(C)(=O)=O)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684129 65369 0 None -8 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 646 14 0 7 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCN(CCCN2CCN(c4ccccc4OC)CC2)S(C)(=O)=O)c1-3 10.1016/j.bmc.2011.01.053
57390119 76078 0 None -218 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 76078 0 None -218 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
44381286 127145 0 None -4 4 Bovine 5.0 pKi = 5.0 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL353220 127145 0 None -4 4 Bovine 5.0 pKi = 5.0 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
118711263 120735 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1ccccc1-c1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
CHEMBL3325914 120735 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1ccccc1-c1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
10432606 211293 0 None -11 2 Rat 6.0 pKi = 6.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 426 7 0 4 4.0 O=C(CCCN1CCN(CC2CC(=O)c3ccc(F)cc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
CHEMBL72649 211293 0 None -11 2 Rat 6.0 pKi = 6.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 426 7 0 4 4.0 O=C(CCCN1CCN(CC2CC(=O)c3ccc(F)cc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
10402195 48300 1 None 1 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3Oc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL149108 48300 1 None 1 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3Oc3ccccc32)CC1 10.1021/jm00030a011
6603798 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL1613539 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL288096 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
117773861 139194 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2ncc(Cl)cc2C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697557 139194 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2ncc(Cl)cc2C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44403213 78562 4 None -1737 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL196744 78562 4 None -1737 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
54581964 68382 0 None -3162 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771111 68382 0 None -3162 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
6603798 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL1613539 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL288096 106956 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
137659303 166083 0 None -154 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 166083 0 None -154 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
118709163 120186 0 None -338 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318835 120186 0 None -338 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12050196 209897 6 None -15 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64043 209897 6 None -15 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
71462090 91368 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2158640 91368 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2221044 91368 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
24949535 188338 0 None -1122 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
CHEMBL476722 188338 0 None -1122 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
177511 108319 23 None -14 2 Rat 5.0 pKi = 5.0 Binding
The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1016/s0960-894x(00)00326-7
CHEMBL298285 108319 23 None -14 2 Rat 5.0 pKi = 5.0 Binding
The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1016/s0960-894x(00)00326-7
156013773 184052 0 None -9 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 280 1 0 3 3.3 CN1CCc2cccc3c2C1Cc1ccc([N+](=O)[O-])cc1-3 10.1016/j.bmcl.2020.127053
CHEMBL4636242 184052 0 None -9 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 280 1 0 3 3.3 CN1CCc2cccc3c2C1Cc1ccc([N+](=O)[O-])cc1-3 10.1016/j.bmcl.2020.127053
1353 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
3559 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
86 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
CHEMBL54 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
DB00502 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
1353 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
3559 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
86 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
CHEMBL54 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
DB00502 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
74223773 136202 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)nc[n+]([O-])c1C nan
CHEMBL3671281 136202 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)nc[n+]([O-])c1C nan
154725276 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4456964 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
25071692 118566 0 None -2187 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 118566 0 None -2187 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
118709169 120193 0 None -6 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318841 120193 0 None -6 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44372009 55613 0 None -123 4 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL155913 55613 0 None -123 4 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
42626103 63027 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 63027 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
44241577 20786 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197140 20786 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL560721 20786 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
117773063 139221 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 4 1 5 4.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697584 139221 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 4 1 5 4.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
154725001 183426 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4525624 183426 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 183426 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
44344506 20600 0 None -8 2 Rat 5.0 pKi = 5.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 327 1 1 2 4.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(-c2ccccc2)c(O)c1-3 10.1021/jm960188q
CHEMBL119577 20600 0 None -8 2 Rat 5.0 pKi = 5.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 327 1 1 2 4.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(-c2ccccc2)c(O)c1-3 10.1021/jm960188q
CHEMBL4802048 220840 0 None - 1 Human 5.0 pKi = 5.0 Binding
GPCRScan assay: inhibition of D1GPCRScan assay: inhibition of D1
ChEMBL None None None CC[C@H](Nc1c(C#N)c(-c2ccc(-c3cccc(C)c3F)cc2)nc2cnccc12)C(=O)O 10.6019/CHEMBL4800729
25139479 191096 0 None -1071 4 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 191096 0 None -1071 4 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
45483655 204894 0 None -138 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
CHEMBL574534 204894 0 None -138 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
71110301 98973 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425371 98973 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL4802048 220840 0 None - 1 Human 5.0 pKi = 5.0 Binding
GPCRScan assay: inhibition of D1GPCRScan assay: inhibition of D1
ChEMBL None None None CC[C@H](Nc1c(C#N)c(-c2ccc(-c3cccc(C)c3F)cc2)nc2cnccc12)C(=O)O 10.6019/CHEMBL4800729
2726 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
621 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
83 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL71 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
DB00477 7706 68 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
127047859 146829 0 None -338 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 146829 0 None -338 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
45481877 204908 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 10 2 10 3.6 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5ncccn5)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
CHEMBL574627 204908 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 10 2 10 3.6 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5ncccn5)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
3082625 201507 8 None -199 4 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2007.05.057
CHEMBL53510 201507 8 None -199 4 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2007.05.057
154705128 183070 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4454872 183070 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 183070 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
100 10577 58 None -47 54 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -47 54 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -47 54 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -47 54 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -47 54 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
86767094 136204 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cncc2nccn12 nan
CHEMBL3671283 136204 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cncc2nccn12 nan
1353 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
3559 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
86 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
CHEMBL54 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
DB00502 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
1353 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
3559 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
86 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
CHEMBL54 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
DB00502 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
1353 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
3559 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
86 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
CHEMBL54 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
DB00502 8692 93 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
10454026 24679 0 None -3019 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
CHEMBL125916 24679 0 None -3019 8 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
10058098 205386 9 None - 1 Rat 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligandCompound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligand
ChEMBL 179 0 3 3 0.8 Oc1cc2c(cc1O)CCNCC2 10.1021/jm00160a018
CHEMBL57873 205386 9 None - 1 Rat 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligandCompound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligand
ChEMBL 179 0 3 3 0.8 Oc1cc2c(cc1O)CCNCC2 10.1021/jm00160a018
11678172 84807 0 None -2137 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 84807 0 None -2137 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
25071384 118558 0 None -251 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 118558 0 None -251 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
44381118 64343 0 None -426 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL166587 64343 0 None -426 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
44319102 212920 0 None -16 4 Bovine 5.0 pKi = 5.0 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 212920 0 None -16 4 Bovine 5.0 pKi = 5.0 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
44582187 188349 0 None -47 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 8 0 4 3.7 COc1ccccc1N1CCN(CCCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476808 188349 0 None -47 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 8 0 4 3.7 COc1ccccc1N1CCN(CCCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
44323870 118368 0 None 3 4 Rat 7.0 pKi = 7.0 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL328246 118368 0 None 3 4 Rat 7.0 pKi = 7.0 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
25142456 89181 2 None -48 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None -48 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44415685 86942 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 551 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213466 86942 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 551 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415450 146401 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 425 1 1 5 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(C)(C)C)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL379757 146401 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 425 1 1 5 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(C)(C)C)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
1353 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
3559 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
86 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
CHEMBL54 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
DB00502 8692 93 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
118445551 174094 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
CHEMBL4294009 174094 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
53363201 70629 0 None -114 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803054 70629 0 None -114 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
71722297 109249 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 109249 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 109249 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
49782601 24260 0 None -602 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1257810 24260 0 None -602 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
10561522 42975 0 None -51 2 Bovine 4.0 pKi = 4.0 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2c(C)cccc2C)C1 10.1021/jm9708700
CHEMBL144501 42975 0 None -51 2 Bovine 4.0 pKi = 4.0 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2c(C)cccc2C)C1 10.1021/jm9708700
154705520 183039 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4452683 183039 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 183039 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
2750 210840 76 None -5 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -5 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
15115519 213986 0 None -151 2 Human 7.0 pKi = 7 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 677 12 1 10 6.4 O=C(CCCN1CCC2(CC1)C(=O)N(CCc1ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc1)CN2c1ccccc1)c1ccc(F)cc1 10.1021/jm00115a012
CHEMBL92649 213986 0 None -151 2 Human 7.0 pKi = 7 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 677 12 1 10 6.4 O=C(CCCN1CCC2(CC1)C(=O)N(CCc1ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc1)CN2c1ccccc1)c1ccc(F)cc1 10.1021/jm00115a012
44415605 86890 0 None 11 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213238 86890 0 None 11 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
42625205 63028 0 None -89 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627324 63028 0 None -89 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
3303 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
5311200 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
CHEMBL267014 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
3303 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
5311200 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
CHEMBL267014 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
24824066 164159 0 None -2 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL407818 164159 0 None -2 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
3303 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 9024 46 None -14791 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
154706703 183011 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4550187 183011 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4594691 183011 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
154725749 183467 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4453478 183467 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598388 183467 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
240 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
3294 8787 111 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2601 10552 33 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
100 10577 58 None -16 54 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -16 54 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -16 54 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -16 54 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -16 54 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5281878 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1028 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 None -91 30 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1960 9632 67 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 9632 67 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 9632 67 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 9632 67 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 9632 67 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
1153 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 8409 58 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2869 10924 89 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60 10924 89 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60857 10924 89 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
CHEMBL1185 10924 89 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
DB00315 10924 89 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
5018 10322 13 None 2 10 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
943 10322 13 None 2 10 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
946 10322 13 None 2 10 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
CHEMBL13668 10322 13 None 2 10 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
None 223163 0 3H-SCH23390 5495 2 Rat 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 329 1 1 3 3.6 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OCC4)O)Cl None
None 223161 0 3H-SCH23390 165 2 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 327 1 1 3 4.4 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OC=C4)O)Cl None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1242 10385 27 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1243 10390 34 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
944 10390 34 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
CHEMBL324017 10390 34 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
5281878 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
25058166 222739 0 3H-SCH23390 High -6 26 Bovine 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 High -6 26 Bovine 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
3036864 209533 19 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5018 10322 13 3H-SCH23390 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
5018 10322 13 UNDEFINED 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 3H-SCH23390 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 UNDEFINED 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 3H-SCH23390 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 UNDEFINED 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 3H-SCH23390 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 UNDEFINED 2 10 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
3036864 209533 19 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
37459 7533 13 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
37459 7533 13 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
133538 10391 24 3H-SCH23390 1 6 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
8443 10391 24 3H-SCH23390 1 6 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
CHEMBL574558 10391 24 3H-SCH23390 1 6 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
3036864 209533 19 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 209533 19 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1218 10388 30 3H-SCH23390 11 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
938 10388 30 3H-SCH23390 11 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
CHEMBL353335 10388 30 3H-SCH23390 11 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
None 223165 0 3H-SCH23390 436 2 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 349 1 2 3 3.3 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O.Br None
277 8083 62 3H-SCH23390 -33 50 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-SCH23390 -33 50 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-SCH23390 -33 50 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-SCH23390 -33 50 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-SCH23390 -33 50 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
135398745 9688 112 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6603820 102549 19 3H-SCH23390 1 12 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 1 12 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1241 106955 24 3H-SCH23390 -1 8 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL288090 106955 24 3H-SCH23390 -1 8 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL552611 106955 24 3H-SCH23390 -1 8 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
135398745 9688 112 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
100 10577 58 3H-SCH23390 -47 54 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SCH23390 -47 54 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SCH23390 -47 54 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SCH23390 -47 54 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SCH23390 -47 54 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
202 8290 77 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 8290 77 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 8290 77 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 8290 77 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 8290 77 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2 10035 23 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
121881 10263 27 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 10263 27 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 10263 27 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
46222048 15756 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 15756 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
18922713 105274 0 3H-SCH23390 -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 105274 0 3H-SCH23390 -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
24840389 121991 4 3H-SCH23390 -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 121991 4 3H-SCH23390 -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
44591098 183541 0 UNDEFINED -288 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL460402 183541 0 UNDEFINED -288 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
12016890 197555 6 3H-SCH23390 -1698 12 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 197555 6 3H-SCH23390 -1698 12 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
5656 209845 87 UNDEFINED -25 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 UNDEFINED -25 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 209906 52 UNDEFINED -1 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 209906 52 UNDEFINED -1 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 222771 0 3H-SCH23390 -107 11 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
104911 222798 0 3H-SCH23390 -4168 37 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
3075702 224111 0 3H-SCH23390 -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1574 6869 60 3H-SCH23390 -107 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 3H-SCH23390 -107 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 3H-SCH23390 -107 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
5 6927 72 3H-SCH23390 Low -23442 53 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-SCH23390 -16595 53 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-SCH23390 Low -23442 53 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-SCH23390 -16595 53 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-SCH23390 Low -23442 53 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-SCH23390 -16595 53 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-SCH23390 Low -23442 53 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-SCH23390 -16595 53 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1192 6935 47 3H-dopamine -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 6935 47 3H-dopamine -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 6935 47 3H-dopamine -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1220 6975 55 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3153 7085 28 3H-SCH23390 Low -39 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 7085 28 3H-SCH23390 Low -39 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 7085 28 3H-SCH23390 Low -39 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
179 7188 115 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
179 7188 115 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2554 7583 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
489 7583 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
5339 7583 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
CHEMBL108 7583 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
DB00564 7583 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
2147 8183 17 3H-SCH23390 -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
5826 8183 17 3H-SCH23390 -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
841 8183 17 3H-SCH23390 -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
CHEMBL612 8183 17 3H-SCH23390 -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
DB01576 8183 17 3H-SCH23390 -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
3016 8194 48 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3364 8194 48 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
852 8194 48 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
CHEMBL12 8194 48 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
DB00829 8194 48 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3151 8244 97 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 8244 97 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 8244 97 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 8244 97 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 8244 97 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
681 8247 72 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681 8247 72 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1209 8439 75 3H-SCH23390 -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 8439 75 3H-SCH23390 -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 8439 75 3H-SCH23390 -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 8439 75 3H-SCH23390 -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 8439 75 3H-SCH23390 -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
1067 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
119 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
1262 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
5410 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
6992099 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
CHEMBL96 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
DB02530 8490 128 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
119376 8622 48 3H-SCH23390 -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-SCH23390 -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-SCH23390 -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1204 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 8713 119 3H-SCH23390 -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
12575 8769 30 3H-SCH23390 -6606 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 8769 30 3H-SCH23390 -6606 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 8769 30 3H-SCH23390 -6606 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
1427 8794 54 3H-dopamine -977 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 8794 54 3H-SCH23390 -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 8794 54 3H-dopamine -977 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 8794 54 3H-SCH23390 -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 8794 54 3H-dopamine -977 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 8794 54 3H-SCH23390 -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 8794 54 3H-dopamine -977 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 8794 54 3H-SCH23390 -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 8794 54 3H-dopamine -977 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 8794 54 3H-SCH23390 -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1310 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
18971832 9196 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 9196 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 9196 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
119192 9259 54 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1582 9259 54 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
CHEMBL506981 9259 54 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
DB06455 9259 54 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1605 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
1728 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
22267 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
4095 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
4586 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
5458 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
CHEMBL159659 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
CHEMBL651 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
DB00333 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
DB13515 9276 24 3H-dopamine -3235 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C None
134 9292 24 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1782 9296 84 3H-SCH23390 -676 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 3H-SCH23390 -676 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 3H-SCH23390 -676 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 3H-SCH23390 -676 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 3H-SCH23390 -676 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1830 9368 44 3H-dopamine -1778 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 9368 44 3H-SCH23390 -1778 28 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-dopamine -1778 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-SCH23390 -1778 28 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-dopamine -1778 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-SCH23390 -1778 28 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-dopamine -1778 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-SCH23390 -1778 28 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-dopamine -1778 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-SCH23390 -1778 28 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1638 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
1676 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
1878 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
5284596 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
CHEMBL80 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
DB01183 9501 38 3H-SCH23390 -5495 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
484 9633 51 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 9633 51 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 9637 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
163839 9729 0 3H-SCH23390 -562 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 9729 0 3H-SCH23390 -562 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 9729 0 3H-SCH23390 -562 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
2136 9869 30 3H-dopamine -2511 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
4768 9869 30 3H-dopamine -2511 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
7268 9869 30 3H-dopamine -2511 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
CHEMBL753 9869 30 3H-dopamine -2511 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
DB00925 9869 30 3H-dopamine -2511 6 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
2142 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-SCH23390 -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-dopamine -3801 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-SCH23390 -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
16362 9899 71 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2202 9906 96 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
119570 9933 96 3H-SCH23390 -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570 9933 96 UNDEFINED -4570 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-SCH23390 -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 UNDEFINED -4570 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-SCH23390 -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 UNDEFINED -4570 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-SCH23390 -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 UNDEFINED -4570 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-SCH23390 -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 UNDEFINED -4570 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2286 9957 51 3H-dopamine -3311 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 9957 51 3H-dopamine -3311 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 9957 51 3H-dopamine -3311 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 9957 51 3H-dopamine -3311 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 9957 51 3H-dopamine -3311 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2303 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 3H-dopamine -21877 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
243 9976 91 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 10035 23 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
2 10035 23 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
173 10036 95 3H-SCH23390 -114 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-SCH23390 -114 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-SCH23390 -114 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
3033769 10054 61 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 10054 61 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
2389 10104 118 3H-SCH23390 -346 66 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -346 66 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -346 66 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -346 66 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -346 66 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2402 10143 62 3H-SCH23390 -61 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-SCH23390 -61 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-SCH23390 -61 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-SCH23390 -61 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-SCH23390 -61 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
183782 10171 20 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
237 10171 20 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL85251 10171 20 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
128563 10237 33 3H-SCH23390 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 3H-SCH23390 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 3H-SCH23390 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 3H-SCH23390 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
221 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
1577 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 3H-SCH23390 -69 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 3H-SCH23390 -537 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 3H-SCH23390 -537 20 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 3H-SCH23390 -537 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1267 10576 49 3H-dopamine -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 10576 49 3H-dopamine -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 10576 49 3H-dopamine -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
102 10899 48 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
6047 11095 110 3H-SCH23390 1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 N[C@@H](Cc1ccc(O)c(O)c1)C(=O)O None
6971033 11095 110 3H-SCH23390 1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 N[C@@H](Cc1ccc(O)c(O)c1)C(=O)O None
CHEMBL1009 11095 110 3H-SCH23390 1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 N[C@@H](Cc1ccc(O)c(O)c1)C(=O)O None
19493 18027 65 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1179 18027 65 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1255743 18027 65 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
2662 18156 131 3H-SCH23390 -3 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 3H-SCH23390 -3 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10836 21239 14 3H-SCH23390 -147 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 21239 14 3H-SCH23390 -147 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
5090 22333 106 3H-SCH23390 -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 3H-SCH23390 -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
671690 33870 35 3H-SCH23390 -10 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
CHEMBL1365455 33870 35 3H-SCH23390 -10 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
10297 33885 30 3H-SCH23390 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 3H-SCH23390 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 53574 99 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 53574 99 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 53574 99 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
53321123 65322 0 UNDEFINED -181 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 0 2 4.2 C#CCOc1cccc2c1-c1cccc3c1C(C2)N(CCC)CC3 None
CHEMBL1684022 65322 0 UNDEFINED -181 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 0 2 4.2 C#CCOc1cccc2c1-c1cccc3c1C(C2)N(CCC)CC3 None
10624 77075 19 3H-SCH23390 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 77075 19 3H-SCH23390 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 77075 19 3H-SCH23390 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
14659268 86413 2 UNDEFINED -134 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 None
CHEMBL2115032 86413 2 UNDEFINED -134 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 None
108107 86719 38 3H-dopamine -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 86719 38 3H-dopamine -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 86719 38 3H-dopamine -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 86719 38 3H-dopamine -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
442108 91411 6 3H-SCH23390 -1 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 91411 6 3H-SCH23390 -1 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
54477 91428 36 3H-SCH23390 -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 91428 36 UNDEFINED -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-SCH23390 -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 UNDEFINED -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
21830793 98610 10 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 98610 10 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 101008 100 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 101008 100 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
44448057 101593 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL253529 101593 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448062 101623 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
CHEMBL253737 101623 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
44448066 101650 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
CHEMBL253948 101650 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
44448068 101651 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 4 0 3 5.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(Cc1ccccc1)CC2 None
CHEMBL253949 101651 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 4 0 3 5.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(Cc1ccccc1)CC2 None
4528 104902 80 3H-SCH23390 -120 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
4528 104902 80 3H-SCH23390 -120 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 104902 80 3H-SCH23390 -120 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 104902 80 3H-SCH23390 -120 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
104870 105656 47 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
3025067 106158 64 3H-dopamine -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 106158 64 3H-dopamine -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 106158 64 3H-dopamine -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
3663 106743 83 3H-SCH23390 -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 106743 83 3H-SCH23390 -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
127708 119298 7 UNDEFINED -251 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 119298 7 UNDEFINED -251 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
3452843 126303 15 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 126303 15 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
446220 140299 14 3H-SCH23390 -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 3H-SCH23390 -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
44208932 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
9669 159967 2 3H-dopamine -3890 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 2 1 2 3.9 CC(C)=CCN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@H]2C None
CHEMBL397705 159967 2 3H-dopamine -3890 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 2 1 2 3.9 CC(C)=CCN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@H]2C None
44448058 161983 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL402517 161983 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448065 162259 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL404037 162259 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
44448069 162309 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 337 4 0 3 4.2 CCCN1CCc2cc(OC)c(OC)c3c2C1Cc1ccccc1C3 None
CHEMBL404241 162309 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 337 4 0 3 4.2 CCCN1CCc2cc(OC)c(OC)c3c2C1Cc1ccccc1C3 None
1615 174570 24 3H-SCH23390 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-SCH23390 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
4595 183494 106 3H-dopamine -186 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 183494 106 3H-dopamine -186 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
44581146 183607 0 UNDEFINED -354 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.5 COc1cccc2cc3n(c12)CCN(CCCCNC(=O)C1=Cc2ccccc2CN1)C3 None
CHEMBL461023 183607 0 UNDEFINED -354 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.5 COc1cccc2cc3n(c12)CCN(CCCCNC(=O)C1=Cc2ccccc2CN1)C3 None
24949694 189549 0 UNDEFINED -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 6 0 7 3.4 c1cnc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
CHEMBL479026 189549 0 UNDEFINED -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 6 0 7 3.4 c1cnc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
43815 193699 64 3H-SCH23390 -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 193699 64 3H-SCH23390 -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 193699 64 3H-SCH23390 -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
11676600 194524 0 UNDEFINED -1174 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 442 6 0 5 4.4 COc1cccc2cc3n(c12)CCN(CCCCN1CCn2c(cc4ccccc42)C1=O)C3 None
CHEMBL495573 194524 0 UNDEFINED -1174 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 442 6 0 5 4.4 COc1cccc2cc3n(c12)CCN(CCCCN1CCn2c(cc4ccccc42)C1=O)C3 None
11704609 194802 0 UNDEFINED -2691 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 427 6 0 5 3.6 N#Cc1cccc(N2CCN(CCCCN3CCn4c(cc5ccccc54)C3=O)CC2)c1 None
CHEMBL497573 194802 0 UNDEFINED -2691 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 427 6 0 5 3.6 N#Cc1cccc(N2CCN(CCCCN3CCn4c(cc5ccccc54)C3=O)CC2)c1 None
11596521 194815 0 UNDEFINED -18620 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 402 7 1 5 3.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
CHEMBL497604 194815 0 UNDEFINED -18620 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 402 7 1 5 3.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
5280343 195054 124 3H-SCH23390 -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 3H-SCH23390 -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 3H-SCH23390 -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
44581147 197153 0 UNDEFINED -1659 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.6 COc1cccc2c1C1CCN(CCCCNC(=O)C3=Cc4ccccc4CN3)CC1=N2 None
CHEMBL517730 197153 0 UNDEFINED -1659 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.6 COc1cccc2c1C1CCN(CCCCNC(=O)C3=Cc4ccccc4CN3)CC1=N2 None
24949388 197307 0 UNDEFINED -6309 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 6 0 6 3.5 c1ccc(N2CCN(CCCSc3nc4ccccc4o3)CC2)nc1 None
CHEMBL517962 197307 0 UNDEFINED -6309 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 6 0 6 3.5 c1ccc(N2CCN(CCCSc3nc4ccccc4o3)CC2)nc1 None
3672 199312 136 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 199312 136 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 200394 112 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 200394 112 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
2771 201796 74 3H-SCH23390 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 201796 74 3H-SCH23390 -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-SCH23390 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-SCH23390 -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-SCH23390 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-SCH23390 -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
4495 203314 92 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 203314 92 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
45112568 205585 0 UNDEFINED -229 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 None
CHEMBL583422 205585 0 UNDEFINED -229 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 None
54677470 207330 115 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 207330 115 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 207330 115 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 209053 22 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3036864 209533 19 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5281600 209804 92 3H-SCH23390 -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-SCH23390 -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 209845 87 3H-SCH23390 -25 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 3H-SCH23390 -25 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 210262 15 3H-SCH23390 -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 210262 15 3H-SCH23390 -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 210262 15 3H-SCH23390 -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
1614 210434 24 3H-SCH23390 -81 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 210434 24 3H-SCH23390 -81 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
202478 211466 20 3H-SCH23390 -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-SCH23390 -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 211497 17 3H-SCH23390 -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 211497 17 3H-SCH23390 -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
5311189 211620 11 3H-SCH23390 -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 211620 11 3H-SCH23390 -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 212120 21 3H-SCH23390 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 212120 21 3H-SCH23390 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 212120 21 3H-SCH23390 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 212280 72 3H-SCH23390 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-SCH23390 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-SCH23390 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
5324346 212361 59 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL1409 212361 59 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL814 212361 59 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
7108 212537 110 3H-SCH23390 -8 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 199 0 1 2 3.9 c1ccc2c(c1)Nc1ccccc1S2 None
CHEMBL828 212537 110 3H-SCH23390 -8 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 199 0 1 2 3.9 c1ccc2c(c1)Nc1ccccc1S2 None
119607 212982 113 3H-SCH23390 -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 212982 113 3H-SCH23390 -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
3337 213146 27 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
444 213445 53 3H-SCH23390 -2089 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
CHEMBL894 213445 53 3H-SCH23390 -2089 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
16231 214288 57 3H-dopamine -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 214288 57 3H-dopamine -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
12057539 214820 42 3H-SCH23390 -18620 21 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 214820 42 3H-SCH23390 -18620 21 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 214820 42 3H-SCH23390 -18620 21 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
6852400 222716 0 3H-dopamine -14125 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
6852400 222716 0 3H-SCH23390 -25118 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
6852400 222716 0 3H-SCH23390 -25118 22 Rhesus macaque 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-dopamine -14125 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-SCH23390 -25118 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-SCH23390 -25118 22 Rhesus macaque 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
57174031 222719 0 3H-SCH23390 -1778 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 222722 0 3H-dopamine -7943 11 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
165193 222724 0 3H-SCH23390 -42657 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
165193 222724 0 3H-SCH23390 -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-SCH23390 -42657 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-SCH23390 -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-SCH23390 -42657 30 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-SCH23390 -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
164512405 222728 0 3H-SCH23390 -457 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
164512405 222728 0 3H-SCH23390 -457 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
11954224 222732 0 3H-SCH23390 -3467 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3246155 222741 0 3H-dopamine -43651 17 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
11954259 222758 0 3H-dopamine -7762 43 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
57525649 222769 0 3H-SCH23390 -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 4 0 1 2.2 CC(CC1=CC=CC=C1)N(C)CC#C None
44134711 222770 0 3H-SCH23390 -112201 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 222771 0 3H-SCH23390 -1071 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
None 222772 0 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
6420041 222773 0 3H-SCH23390 -14 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 4 0 2 3.8 CN(C)CC=C(C1=CC=C(C=C1)Br)C2=CN=CC=C2 None
104911 222798 0 3H-SCH23390 -41686 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 222806 0 3H-SCH23390 -6309 13 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 453 9 2 6 2.6 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CCNS(=O)(=O)C)Cl)N.Cl None
131632304 222816 0 3H-SCH23390 -70794 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
119380 222908 0 125I-SCH 23982 -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 166 1 0 3 1.8 CC1=NOC(=C1)C2CCCN2C None
None 222914 0 3H-SCH23390 -10471 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
25137849 222958 0 3H-SCH23390 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-SCH23390 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223013 0 3H-SCH23390 -13 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
None 223018 0 3H-SCH23390 -95499 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 223033 0 3H-dopamine -8317 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
5372683 223065 0 3H-dopamine -1479 3 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 400 5 1 4 4.2 C1CN(CCN1CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO None
None 223090 0 3H-SCH23390 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 223091 0 3H-SCH23390 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-SCH23390 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 223093 0 3H-SCH23390 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 223094 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 223095 0 3H-SCH23390 -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 3H-SCH23390 -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223097 0 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 223104 0 3H-SCH23390 -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 3H-SCH23390 -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
4978 223107 0 3H-SCH23390 -7 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 223108 0 3H-SCH23390 -3 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 223109 0 3H-SCH23390 -281 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 223110 0 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 223121 0 3H-SCH23390 -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 223168 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 223169 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 223170 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 223171 0 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 223172 0 3H-SCH23390 -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 223173 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 223174 0 3H-SCH23390 -7 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 223229 0 UNDEFINED -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 223229 0 UNDEFINED -660 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 223268 0 3H-SCH23390 -4570 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
None 223273 0 3H-SCH23390 -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
None 223346 0 UNDEFINED -549 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
None 223499 0 UNDEFINED -3090 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 3.1 CC1=C(C2=C(CC3C4=C2C=CC=C4CCN3)C=C1)O None
None 223501 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 601 23 0 3 11.9 CCCCCCCCCCCCCCCCCCCCCC(=O)OC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)CCC None
None 223502 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 363 6 0 3 5.3 CCCCC(=O)OC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)CCC None
None 223503 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 3 0 3 4.1 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC(=O)C None
None 223511 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 4.1 CCCN1CCC2=C3C1CC4=C(C=CC(=C4)O)OC3=CC=C2 None
None 223512 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 4.1 CCCN1CCC2=CC(=CC3=C2C1CC4=CC=CC=C4O3)O None
None 223551 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 323 4 1 3 4.3 CCCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
None 223939 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 436 9 2 5 4.7 CCCN(CCCCNC(=O)C1=CC2=CC=CC=C2C=C1)C3CCC4=C(C3)SC(=N4)N None
None 224051 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 4 0 4 4.2 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)OC(=O)C None
None 224052 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 0 4 5.3 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)CCC)OC None
None 224294 0 UNDEFINED -1023 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 0 0 2 3.8 CC1CC2=C(O1)C3=C(CC4C5=C3C=CC=C5CCN4C)C=C2 None
None 224295 0 UNDEFINED -69 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 3 1 3 3.9 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)CC=C)O None
None 224296 0 UNDEFINED -151 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 0 3 4.0 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)OCC=C None
None 224297 0 UNDEFINED -346 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 0 0 2 4.5 CC1=CC2=C(O1)C3=C(CC4C5=C3C=CC=C5CCN4C)C=C2 None
None 224298 0 UNDEFINED -707 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 2 0 2 3.5 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC#C None
None 224299 0 UNDEFINED -74 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 2 1 2 3.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC=C)O None
None 224300 0 UNDEFINED -831 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 3 0 2 4.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C None
None 224301 0 UNDEFINED -19 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 0 2 5.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(C=C4)C(=C(O5)C)C None
None 224302 0 UNDEFINED -30 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 2 0 2 5.3 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(C=C4)C=C(O5)C None
None 224303 0 UNDEFINED -79 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 2 4.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC#CC None
None 224304 0 UNDEFINED -15 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 2 0 2 4.9 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(CC(O5)(C)C)C=C4 None
None 224305 0 UNDEFINED -12 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 4 1 2 4.7 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC=C)O None
None 224306 0 UNDEFINED -67 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 5 0 2 5.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C(C)C None
None 224307 0 UNDEFINED -26 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 5 0 2 5.2 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC(=C)C None
None 224308 0 UNDEFINED -35 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 5 0 2 4.8 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C None
None 224316 0 UNDEFINED 1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 4 1 2 5.4 CCCN1CCC2=CC=CC3=C2C1CC4=C(C=CC(=C43)O)CC=C(C)C None
None 224317 0 UNDEFINED 1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 5.0 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC(=C)C)O None
1524 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-SCH23390 -338 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
25058166 222739 0 UNDEFINED -147 26 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 UNDEFINED -147 26 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
126968774 222768 0 3H-dopamine -42 8 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O None
1242 10385 27 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1353 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
45112462 203745 0 UNDEFINED -831 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 None
CHEMBL566533 203745 0 UNDEFINED -831 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 None
25058166 222739 0 3H-SCH23390 Low -6 26 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 Low -6 26 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
3153 7085 28 3H-dopamine -39 8 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 7085 28 3H-dopamine -39 8 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 7085 28 3H-dopamine -39 8 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
1212 8443 50 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
681 8247 72 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223498 0 UNDEFINED -190 2 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 237 0 2 2 2.8 C1CNC2CC3=C(C4=C2C1=CC=C4)C(=CC=C3)O None
2726 7706 68 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1218 10388 30 3H-SCH23390 -11 8 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
938 10388 30 3H-SCH23390 -11 8 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
CHEMBL353335 10388 30 3H-SCH23390 -11 8 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
2726 7706 68 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
None 223738 0 UNDEFINED 1 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 365 5 0 4 4.5 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
277 8083 62 3H-SCH23390 -33 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-SCH23390 -33 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-SCH23390 -33 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-SCH23390 -33 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-SCH23390 -33 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1353 8692 93 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2435 10362 83 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1353 8692 93 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
277 8083 62 3H-dopamine -1445 50 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-dopamine -1445 50 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-dopamine -1445 50 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-dopamine -1445 50 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-dopamine -1445 50 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4508 9913 98 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4866774 9913 98 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
509 9913 98 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
838 9913 98 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
CHEMBL1740 9913 98 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4249 84954 34 3H-dopamine -1230 6 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 84954 34 3H-dopamine -1230 6 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
681 8247 72 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 224144 0 UNDEFINED - 1 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 409 2 3 4 5.0 CCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O.Cl None
2337 10030 77 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
24949690 188385 0 UNDEFINED -1819 3 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 None
CHEMBL477200 188385 0 UNDEFINED -1819 3 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 None
2337 10030 77 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
681 8247 72 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 10915 73 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 223553 0 UNDEFINED - 1 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.5 CCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
2337 10030 77 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2865 10915 73 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 224142 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 331 1 2 3 4.0 CCN1CCC2=C3C1CC4=C(C3=CC(=C2)C)C(=C(C=C4)O)O.Cl None
1242 10385 27 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
2105 9828 37 3H-SCH23390 -123 32 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-SCH23390 -123 32 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-SCH23390 -123 32 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-SCH23390 -123 32 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-SCH23390 -123 32 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
135409468 8816 69 3H-SCH23390 -12 39 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-SCH23390 -12 39 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-SCH23390 -12 39 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
37459 7533 13 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1222 8445 49 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 10425 50 3H-dopamine -31622 58 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-dopamine -31622 58 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-dopamine -31622 58 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-dopamine -31622 58 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-dopamine -31622 58 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135398737 7745 93 3H-SCH23390 -44 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -44 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -44 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -44 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -44 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
127708 119298 7 UNDEFINED -22 5 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 119298 7 UNDEFINED -22 5 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
135 9310 43 3H-SCH23390 -91 56 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-SCH23390 -91 56 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-SCH23390 -91 56 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-SCH23390 -91 56 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-SCH23390 -91 56 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
16362 9899 71 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
681 8247 72 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
2389 10104 118 3H-SCH23390 -489 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -489 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -489 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -489 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -489 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 223738 0 UNDEFINED -12 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 365 5 0 4 4.5 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
1353 8692 93 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223514 0 UNDEFINED - 1 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 419 3 1 5 3.9 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O)Br None
1242 10385 27 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1890 9535 49 3H-SCH23390 -234 16 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 9535 49 3H-SCH23390 -234 16 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 9535 49 3H-SCH23390 -234 16 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 9535 49 3H-SCH23390 -234 16 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 9535 49 3H-SCH23390 -234 16 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
11954259 222758 0 3H-SCH23390 -5011 43 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
71299720 222730 0 3H-SCH23390 -1202 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1353 8692 93 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
134 9292 24 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1613 9127 53 3H-SCH23390 -4 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SCH23390 -4 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SCH23390 -4 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SCH23390 -4 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SCH23390 -4 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
681 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
33630 185736 99 3H-dopamine -281 28 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 185736 99 3H-dopamine -281 28 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
24949534 196297 0 UNDEFINED -2041 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 None
CHEMBL514074 196297 0 UNDEFINED -2041 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 None
11653679 187970 1 UNDEFINED -24 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 187970 1 UNDEFINED -24 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
None 223552 0 UNDEFINED - 1 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 3 1 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
5018 10322 13 3H-SCH23390 -28 10 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 3H-SCH23390 -28 10 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 3H-SCH23390 -28 10 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 3H-SCH23390 -28 10 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
172286 223166 0 3H-SCH23390 1 2 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 331 0 0 4 3.6 CN1CCN(CC1)C2=NC3=C(CC4=C2C=CS4)C=CC(=C3)Cl None
681 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 223161 0 3H-SCH23390 165 2 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 1 1 3 4.4 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OC=C4)O)Cl None
None 223505 0 UNDEFINED - 1 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 343 1 2 3 4.5 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=CC=C4)O)C5=CC=C(C=C5)O None
15443 124588 96 3H-dopamine -257 10 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 None
CHEMBL340211 124588 96 3H-dopamine -257 10 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 None
5018 10322 13 3H-SCH23390 -28 10 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 3H-SCH23390 -28 10 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 3H-SCH23390 -28 10 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 3H-SCH23390 -28 10 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
3036864 209533 19 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
2286 9957 51 3H-SCH23390 -588 30 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 9957 51 3H-SCH23390 -588 30 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 9957 51 3H-SCH23390 -588 30 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 9957 51 3H-SCH23390 -588 30 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 9957 51 3H-SCH23390 -588 30 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
100 10577 58 3H-dopamine -309 54 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-dopamine -309 54 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-dopamine -309 54 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-dopamine -309 54 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-dopamine -309 54 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1212 8443 50 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11976 7707 59 UNDEFINED -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 7707 59 UNDEFINED -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 7707 59 UNDEFINED -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 7707 59 UNDEFINED -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1212 8443 50 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1242 10385 27 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1242 10385 27 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 8443 50 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1621 9207 17 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
None 223061 0 3H-dopamine 2 2 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 1 2 2 1.5 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)N None
100 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 223509 0 UNDEFINED - 1 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 325 3 2 4 3.6 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O None
100 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-dopamine -309 54 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
30137 9652 0 3H-SCH23390 -676 9 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 9652 0 3H-SCH23390 -676 9 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 9652 0 3H-SCH23390 -676 9 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
1153 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 8409 58 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 223149 0 3H-SCH23390 -11220 2 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 487 8 2 4 3.9 CNC1=C(C=C(C(=C1)OC)C(=O)NCCN(C)CC2=CC=C(C=C2)I)Cl None
135398737 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1524 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-SCH23390 -79 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
None 223063 0 3H-dopamine -741 2 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 454 6 1 4 4.8 C1CN(CCN1CCCC2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F)CCO None
135398737 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -44 90 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
242 7258 124 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 7258 124 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4106 9280 22 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 223517 0 UNDEFINED - 1 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 453 2 2 5 3.5 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)I None
37459 7533 13 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
6603820 102549 19 3H-SCH23390 1 12 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 1 12 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1238 209953 24 3H-SCH23390 -5 16 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 209953 24 3H-SCH23390 -5 16 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
3153 7085 28 3H-SCH23390 High -39 8 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 7085 28 3H-SCH23390 High -39 8 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 7085 28 3H-SCH23390 High -39 8 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
46780481 114308 20 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
20840341 222956 0 3H-SCH23390 -3 4 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 451 5 1 3 6.2 C1CN(CCC1CCO)CCC=C2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F None
6603820 102549 19 3H-SCH23390 -2 12 Rhesus macaque 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 -2 12 Rhesus macaque 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1524 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-SCH23390 -338 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
484 9633 51 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
None 223500 0 UNDEFINED -165 2 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 4.2 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)C)O None
24949857 188546 0 UNDEFINED -7413 3 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 None
CHEMBL477765 188546 0 UNDEFINED -7413 3 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 None
25212275 181200 0 UNDEFINED -4897 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL455288 181200 0 UNDEFINED -4897 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
25212276 196845 0 UNDEFINED -575 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL517244 196845 0 UNDEFINED -575 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
3151 8244 97 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 8244 97 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 8244 97 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 8244 97 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 8244 97 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
135398737 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-dopamine -204 90 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
126968774 222768 0 3H-SCH23390 -831 8 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O None
5475158 73987 25 3H-SCH23390 -489 14 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 73987 25 3H-SCH23390 -489 14 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
1212 8443 50 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 10104 118 UNDEFINED -346 66 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 UNDEFINED -346 66 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 UNDEFINED -346 66 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 UNDEFINED -346 66 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 UNDEFINED -346 66 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 10577 58 3H-SCH23390 -16 54 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SCH23390 -16 54 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SCH23390 -16 54 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SCH23390 -16 54 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SCH23390 -16 54 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
6603820 102549 19 3H-SCH23390 -4 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 -4 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
None 223164 0 125I-SCH 23982 74 2 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 365 2 3 4 3.7 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN.Cl None
4106 9280 22 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2435 10362 83 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
25058166 222739 0 UNDEFINED -147 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 UNDEFINED -147 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 223515 0 UNDEFINED - 1 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 481 4 0 5 4.1 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC)I None
None 223120 0 3H-SCH23390 -281 19 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
3294 8787 111 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
134 9292 24 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
None 223012 0 3H-SCH23390 -3090 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 315 6 1 3 4.3 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O None
2398 7741 62 3H-SCH23390 -11 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 7741 62 3H-SCH23390 -11 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 7741 62 3H-SCH23390 -11 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 7741 62 3H-SCH23390 -11 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 7741 62 3H-SCH23390 -11 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
10742 10389 31 3H-SCH23390 -2 8 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
1225 10389 31 3H-SCH23390 -2 8 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
CHEMBL35354 10389 31 3H-SCH23390 -2 8 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
2470 10425 50 3H-SCH23390 -4168 58 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -4168 58 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -4168 58 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -4168 58 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -4168 58 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4382 111557 31 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
86470 111557 31 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
CHEMBL1256484 111557 31 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
CHEMBL31088 111557 31 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
1212 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 10104 118 3H-SCH23390 -346 66 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -346 66 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -346 66 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -346 66 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -346 66 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
44591134 182979 0 UNDEFINED -194 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459373 182979 0 UNDEFINED -194 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
681 8247 72 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1212 8443 50 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
46780481 114308 20 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 223506 0 UNDEFINED - 1 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 341 3 1 5 3.2 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O None
1212 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2181 9902 46 3H-SCH23390 -2041 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 3H-SCH23390 -2041 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 3H-SCH23390 -2041 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 3H-SCH23390 -2041 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 3H-SCH23390 -2041 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
None 223940 0 UNDEFINED -158 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 532 10 0 4 8.0 CN(CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl)CC4=CC=C(C=C4)OCCCN5CCCCC5 None
2726 7706 68 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1353 8692 93 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11976 7707 59 3H-dopamine -234 24 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 7707 59 3H-dopamine -234 24 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 7707 59 3H-dopamine -234 24 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 7707 59 3H-dopamine -234 24 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135 9310 43 3H-dopamine -457 56 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-dopamine -457 56 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-dopamine -457 56 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-dopamine -457 56 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-dopamine -457 56 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 223739 0 UNDEFINED -7 2 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 339 0 3 6 3.0 CN1CCC2=C3C1CC4=C(C3=CC5=C2SC(=N5)N)C(=C(C=C4)O)O None
None 223555 0 UNDEFINED 1 4 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 251 0 1 2 3.1 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O None
1242 10385 27 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
73333 12735 31 UNDEFINED -16 9 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 12735 31 UNDEFINED -16 9 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
4452 9538 19 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 9538 19 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 9538 19 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
2337 10030 77 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398737 7745 93 3H-SCH23390 -37 90 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -37 90 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -37 90 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -37 90 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -37 90 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 10104 118 3H-SCH23390 -489 66 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -489 66 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -489 66 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -489 66 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -489 66 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 8692 93 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223497 0 UNDEFINED -60 2 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 1 0 1 4.0 CCC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)C None
None 222717 0 3H-SCH23390 -45708 21 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 224145 0 UNDEFINED - 1 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 345 2 2 3 4.4 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)C)C(=C(C=C4)O)O.Cl None
1153 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 8409 58 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2601 10552 33 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1028 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 3H-dopamine -52 30 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
135398737 7745 93 3H-dopamine -204 90 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-dopamine -204 90 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-dopamine -204 90 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-dopamine -204 90 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-dopamine -204 90 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
125564 7453 97 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
388 7453 97 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
7670 7453 97 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
CHEMBL178803 7453 97 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
DB09223 7453 97 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
135398737 7745 93 3H-SCH233930 -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH233930 -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH233930 -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH233930 -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH233930 -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 9831 97 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
135398737 7745 93 UNDEFINED -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -44 90 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
134 9292 24 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
25058166 222739 0 UNDEFINED -144 26 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 UNDEFINED -144 26 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 223508 0 UNDEFINED - 1 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.9 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O None
10145 223507 0 UNDEFINED - 1 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 355 4 0 5 3.5 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC None
None 223736 0 UNDEFINED -1 2 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 265 0 2 3 2.6 CN1CCC2=C3C1CC4=C(C3=CC(=C2)N)C(=CC=C4)N None
185 10778 60 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
122324 6993 22 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
6077 6993 22 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
CHEMBL86931 6993 22 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
37459 7533 13 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
5281878 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
9861622 206223 5 3H-SCH23390 1202 2 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 None
CHEMBL59139 206223 5 3H-SCH23390 1202 2 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 None
62865 8057 0 3H-SCH23390 -2 15 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 8057 0 3H-SCH23390 -2 15 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 8057 0 3H-SCH23390 -2 15 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 8057 0 3H-SCH23390 -2 15 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 8057 0 3H-SCH23390 -2 15 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
1621 9207 17 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2865 10915 73 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11954224 222732 0 3H-dopamine -426 59 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1242 10385 27 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1427 8794 54 3H-SCH23390 -295 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 8794 54 3H-SCH23390 -295 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 8794 54 3H-SCH23390 -295 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 8794 54 3H-SCH23390 -295 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 8794 54 3H-SCH23390 -295 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
10333195 54960 0 UNDEFINED -10 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
CHEMBL155208 54960 0 UNDEFINED -10 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
44591099 182969 0 UNDEFINED -1122 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459350 182969 0 UNDEFINED -1122 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
135398745 9688 112 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 224143 0 UNDEFINED - 1 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 393 2 2 3 5.3 CCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5.Cl None
1353 8692 93 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135 9310 43 3H-SCH23390 -457 56 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-SCH23390 -457 56 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-SCH23390 -457 56 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-SCH23390 -457 56 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-SCH23390 -457 56 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
6852400 222716 0 3H-SCH23390 -14125 22 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-SCH23390 -14125 22 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
186 8588 52 3H-SCH23390 -53 17 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 8588 52 3H-SCH23390 -53 17 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 8588 52 3H-SCH23390 -53 17 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
11696813 194697 12 UNDEFINED -316 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
CHEMBL496739 194697 12 UNDEFINED -316 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
6603820 102549 19 125I-SCH 23982 -4 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 125I-SCH 23982 -4 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2865 10915 73 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2105 9828 37 3H-SCH23390 -123 32 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-SCH23390 -123 32 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-SCH23390 -123 32 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-SCH23390 -123 32 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-SCH23390 -123 32 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1212 8443 50 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 223346 0 UNDEFINED -549 6 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
30137 9652 0 UNDEFINED -3981 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 9652 0 UNDEFINED -3981 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 9652 0 UNDEFINED -3981 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
135398745 9688 112 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6603820 102549 19 3H-SCH23390 -4 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 -4 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10707972 175835 0 UNDEFINED 1 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
CHEMBL439639 175835 0 UNDEFINED 1 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 UNDEFINED -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -83 90 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2470 10425 50 3H-SCH23390 -51286 58 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -51286 58 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -51286 58 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -51286 58 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -51286 58 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 8692 93 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
73453 36389 24 3H-dopamine -51 17 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
CHEMBL1385840 36389 24 3H-dopamine -51 17 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
2470 10425 50 3H-SCH23390 -10964 58 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -10964 58 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -10964 58 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -10964 58 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -10964 58 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25293 222744 0 3H-dopamine -724 4 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 443 6 1 3 5.4 C1CN(CCC1(C2=CC(=C(C=C2)Cl)C(F)(F)F)O)CCCC(=O)C3=CC=C(C=C3)F None
44448059 101595 0 UNDEFINED 5 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
CHEMBL253530 101595 0 UNDEFINED 5 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
25058166 222739 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
213 10625 55 3H-SCH23390 -12 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 3H-SCH23390 -12 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 3H-SCH23390 -12 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 3H-SCH23390 -12 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 3H-SCH23390 -12 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
681 8247 72 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
13994416 197469 1 UNDEFINED -851 2 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1C(C2)N(C)CC3 None
CHEMBL5181992 197469 1 UNDEFINED -851 2 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1C(C2)N(C)CC3 None
5018 10322 13 3H-SCH23390 -194 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 3H-SCH23390 -194 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 3H-SCH23390 -194 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 3H-SCH23390 -194 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
5770 211837 82 3H-SCH23390 -2 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
CHEMBL772 211837 82 3H-SCH23390 -2 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
242 7258 124 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2337 10030 77 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1524 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-SCH23390 -301 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5281878 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
37459 7533 13 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1577 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 None -69 20 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5281878 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2402 10143 62 None -61 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 None -61 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 None -61 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 None -61 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 None -61 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1212 8443 50 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 8443 50 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
10742 10389 31 3H-SCH23390 2 8 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
1225 10389 31 3H-SCH23390 2 8 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
CHEMBL35354 10389 31 3H-SCH23390 2 8 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
6603820 102549 19 3H-SCH23390 1 12 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 1 12 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2662 18156 131 None -3 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 None -3 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
441383 27105 57 None -12 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 27105 57 None -12 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
28417 46813 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 46813 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
2105 9828 37 3H-SCH23390 -147 32 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2105 9828 37 3H-SCH23390 -147 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-SCH23390 -147 32 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-SCH23390 -147 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-SCH23390 -147 32 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-SCH23390 -147 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-SCH23390 -147 32 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-SCH23390 -147 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-SCH23390 -147 32 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-SCH23390 -147 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
25058166 222739 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
4011 89183 49 UNDEFINED -64 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 89183 49 UNDEFINED -64 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
135398737 7745 93 3H-SCH23390 -169 90 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -169 90 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -169 90 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -169 90 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -169 90 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5018 10322 13 3H-SCH23390 2 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 10322 13 3H-SCH23390 2 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 10322 13 3H-SCH23390 2 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 10322 13 3H-SCH23390 2 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
115237 62359 119 3H-SCH23390 -74 54 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-SCH23390 -74 54 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1242 10385 27 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
242 7258 124 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
16363 7383 53 3H-dopamine -20892 7 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 7383 53 3H-dopamine -20892 7 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 7383 53 3H-dopamine -20892 7 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 7383 53 3H-dopamine -20892 7 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 7383 53 3H-dopamine -20892 7 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 9899 71 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
1816 9318 102 3H-SCH23390 -323 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 9318 102 3H-SCH23390 -323 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 9318 102 3H-SCH23390 -323 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 9318 102 3H-SCH23390 -323 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 9318 102 3H-SCH23390 -323 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
3294 8787 111 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2337 10030 77 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135 9310 43 3H-MIANSERIN -91 56 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-MIANSERIN -91 56 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-MIANSERIN -91 56 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-MIANSERIN -91 56 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-MIANSERIN -91 56 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448070 101668 0 UNDEFINED 3 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 None
CHEMBL254147 101668 0 UNDEFINED 3 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 None
25186021 194803 0 UNDEFINED -1318 3 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 None
CHEMBL497574 194803 0 UNDEFINED -1318 3 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 None
25058166 222739 0 3H-SCH23390 -147 26 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 -147 26 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
11712530 194669 0 UNDEFINED -41686 4 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 None
CHEMBL496531 194669 0 UNDEFINED -41686 4 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 None
2726 7706 68 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
209 9831 97 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
None 223346 0 UNDEFINED -549 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
681 8247 72 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1222 8445 49 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 222750 0 3H-SCH23390 -9772 15 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
2337 10030 77 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 9688 112 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 223554 0 UNDEFINED 1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.2 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
None 223554 0 UNDEFINED -1 4 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.2 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
25186569 183761 0 UNDEFINED -45708 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 None
CHEMBL462508 183761 0 UNDEFINED -45708 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 None
None 223011 0 3H-SCH23390 -11 4 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 226 0 2 2 1.4 C1CCC(=O)NCCCCCC(=O)NCC1 None
1524 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-SCH23390 -79 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
219050 10146 25 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 10146 25 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 10146 25 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
5281878 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
30137 9652 0 3H-SCH23390 -1202 9 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 9652 0 3H-SCH23390 -1202 9 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 9652 0 3H-SCH23390 -1202 9 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
6446379 223064 0 3H-dopamine -154 2 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 472 5 1 4 5.1 C1CN(CCN1CC/C=C/2\C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO.Cl.Cl None
10264969 55069 0 UNDEFINED -6 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
CHEMBL155352 55069 0 UNDEFINED -6 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
None 223518 0 UNDEFINED - 1 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 405 2 2 5 3.6 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Br None
2181 9902 46 3H-dopamine -4073 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 3H-dopamine -4073 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 3H-dopamine -4073 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 3H-dopamine -4073 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 3H-dopamine -4073 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
None 223346 0 UNDEFINED -549 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
46780481 114308 20 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
64143 205643 62 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
CHEMBL584 205643 62 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
2477 7532 59 None -28 29 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 None -28 29 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 None -28 29 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 None -28 29 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 None -28 29 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2780 117306 36 None -138 10 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 None -138 10 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
176 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3198 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 212292 76 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2812 11551 101 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1016 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 10519 78 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1816 9318 102 None -323 18 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 9318 102 None -323 18 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 9318 102 None -323 18 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 9318 102 None -323 18 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 9318 102 None -323 18 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
1816 9318 102 None -323 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 9318 102 None -323 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 9318 102 None -323 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 9318 102 None -323 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 9318 102 None -323 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
448537 167029 89 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 167029 89 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
4189 213701 96 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 213701 96 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 213701 96 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1042 8362 23 None -204 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 8362 23 None -204 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 8362 23 None -204 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 8362 23 None -204 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 8362 23 None -204 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
2407 10145 76 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 10145 76 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 10145 76 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 10145 76 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 10145 76 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
5353853 24758 47 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 24758 47 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 24758 47 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
11154555 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 7587 62 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
2247 7293 81 None -61 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 None -61 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 None -61 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 None -61 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 None -61 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
12488 8438 56 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 8438 56 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 8438 56 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 8438 56 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
2351 10059 64 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 10059 64 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 10059 64 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 10059 64 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 10059 64 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
240 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
1830 9368 44 None -16 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 None -16 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 None -16 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 None -16 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 None -16 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
None 223162 0 3H-SCH23390 1737 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 2 1 5 2.9 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OCC4)O)[N+](=O)[O-] None
11057 182928 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 182928 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 182928 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 182928 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
135 9310 43 None -46 56 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -46 56 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -46 56 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -46 56 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -46 56 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2286 9957 51 None -30 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 9957 51 None -30 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 9957 51 None -30 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 9957 51 None -30 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 9957 51 None -30 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2600 10551 74 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 10551 74 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 10551 74 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 10551 74 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 10551 74 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
6917970 10463 61 3H-SCH23390 -1 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 10463 61 3H-SCH23390 -1 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 10463 61 3H-SCH23390 -1 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
2284 9956 33 None -36 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 9956 33 None -36 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 9956 33 None -36 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 9956 33 None -36 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 9956 33 None -36 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
10531 8202 21 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 8202 21 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 8202 21 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 8202 21 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 8202 21 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
3117 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
2389 10104 118 UNDEFINED -346 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 UNDEFINED -346 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 UNDEFINED -346 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 UNDEFINED -346 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 UNDEFINED -346 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3947 213174 53 3H-SCH23390 -74 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 213174 53 3H-SCH23390 -74 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
5 6927 72 3H-SCH23390 -16595 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-SCH23390 -16595 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-SCH23390 -16595 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-SCH23390 -16595 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 223013 0 3H-SCH23390 -6 6 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
None 223013 0 3H-SCH23390 -6 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
11954259 222758 0 3H-SCH23390 -169 43 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
681 8247 72 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
115237 62359 119 3H-SCH23390 -2511 54 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-SCH23390 -2511 54 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
3153 7085 28 3H-SCH23390 -3019 8 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 7085 28 3H-SCH23390 -3019 8 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 7085 28 3H-SCH23390 -3019 8 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
135398745 9688 112 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
31116 223062 0 3H-dopamine -37 2 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 609 5 3 6 2.6 CC(C)C1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398745 9688 112 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223516 0 UNDEFINED - 1 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 433 4 0 5 4.2 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC)Br None
2389 10104 118 3H-SCH23390 -489 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -489 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -489 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -489 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -489 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 224050 0 UNDEFINED - 1 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 323 2 0 4 3.4 CC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
135398737 7745 93 UNDEFINED -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5568 204279 29 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
66069 204279 29 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL1201102 204279 29 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL570 204279 29 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
16362 9899 71 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
185 10778 60 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
135398737 7745 93 3H-SCH23390 -44 90 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -44 90 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -44 90 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -44 90 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -44 90 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 9127 53 3H-SCH23390 -5 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SCH23390 -5 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SCH23390 -5 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SCH23390 -5 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SCH23390 -5 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954259 222758 0 3H-dopamine -7762 43 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
None 223346 0 UNDEFINED -549 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
3294 8787 111 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2995 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
135398737 7745 93 3H-SCH23390 -22 90 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -22 90 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -22 90 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -22 90 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -22 90 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 10104 118 3H-SCH23390 -346 66 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -346 66 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -346 66 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -346 66 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -346 66 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11654739 183627 0 UNDEFINED -20417 4 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 None
CHEMBL461236 183627 0 UNDEFINED -20417 4 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 None
1242 10385 27 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
24949693 189083 0 UNDEFINED -7244 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
CHEMBL478413 189083 0 UNDEFINED -7244 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 10104 118 3H-SCH233930 -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH233930 -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH233930 -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH233930 -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH233930 -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2470 10425 50 3H-SCH23390 -4168 58 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -4168 58 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -4168 58 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -4168 58 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -4168 58 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 8692 93 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2389 10104 118 UNDEFINED -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 UNDEFINED -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 UNDEFINED -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 UNDEFINED -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 UNDEFINED -489 66 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 10577 58 3H-SCH23390 -16 54 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SCH23390 -16 54 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SCH23390 -16 54 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SCH23390 -16 54 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SCH23390 -16 54 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1353 8692 93 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 223106 0 3H-SCH23390 16 27 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
135 9310 43 None -91 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -91 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -91 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -91 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -91 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 223513 0 UNDEFINED - 1 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 467 3 1 5 3.8 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O)I None
11954224 222732 0 None -3467 59 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
242 7258 124 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
26987 7736 33 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 7736 33 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 7736 33 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 7736 33 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 7736 33 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2585 7590 103 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
31101 7516 40 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
6603820 102549 19 3H-SCH23390 1 12 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 1 12 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
3191 109635 97 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 109635 97 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
107715 207724 22 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 207724 22 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 207724 22 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
3168 16034 92 None -89 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 None -89 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
150 9287 21 None -43 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 9287 21 None -43 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 9287 21 None -43 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 9287 21 None -43 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 9287 21 None -43 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
2407 10145 76 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 10145 76 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 10145 76 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 10145 76 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 10145 76 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
5440 35497 37 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
CHEMBL1378 35497 37 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
4011 89183 49 None -64 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 89183 49 None -64 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
134 9292 24 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1530 8963 50 None -53 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 8963 50 None -53 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 8963 50 None -53 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 8963 50 None -53 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 8963 50 None -53 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
68663 34055 23 None -6 4 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 None
CHEMBL136711 34055 23 None -6 4 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 None
135398737 7745 93 None -204 90 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -204 90 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -204 90 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -204 90 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -204 90 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 None -37 90 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -37 90 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -37 90 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -37 90 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -37 90 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2337 10030 77 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
7077 73733 27 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 73733 27 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL3925724 73733 27 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
2105 9828 37 None -123 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 None -123 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 None -123 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 None -123 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 None -123 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2470 10425 50 None -4168 58 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 None -4168 58 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 None -4168 58 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 None -4168 58 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 None -4168 58 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3561 25849 39 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 25849 39 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
1971 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
5462328 224516 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
Drug Central 369 2 0 6 2.0 CN1CC[C@]23[C@H]4OC5=C(OC(C)=O)C=CC(C[C@@H]1[C@@H]2C=C[C@@H]4OC(C)=O)=C35 None
2398 7741 62 None -11 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 7741 62 None -11 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 7741 62 None -11 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 7741 62 None -11 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 7741 62 None -11 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
3294 8787 111 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2435 10362 83 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
134551 7146 27 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 7146 27 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 7146 27 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 7146 27 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
37 7565 60 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 7565 60 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 7565 60 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 7565 60 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 7565 60 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
1524 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 None -79 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
191 7191 98 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1621 9207 17 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11978813 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
681 8247 72 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
33630 185736 99 None -5 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 185736 99 None -5 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
52919 21222 48 None -15 4 Pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1200986 21222 48 None -15 4 Pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
135398737 7745 93 None -44 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -44 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -44 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -44 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -44 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
277 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1712 9270 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 9270 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 9270 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 9270 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 9270 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2389 10104 118 3H-SCH23390 -489 66 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -489 66 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -489 66 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -489 66 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -489 66 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2448 106099 70 3H-dopamine -426 18 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 106099 70 3H-dopamine -426 18 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
1042 8362 23 3H-dopamine -97 17 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 8362 23 3H-dopamine -97 17 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 8362 23 3H-dopamine -97 17 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 8362 23 3H-dopamine -97 17 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 8362 23 3H-dopamine -97 17 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
None 223555 0 UNDEFINED -2 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 251 0 1 2 3.1 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O None
10265732 101624 0 UNDEFINED 2 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL253738 101624 0 UNDEFINED 2 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
2389 10104 118 3H-SCH23390 -346 66 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -346 66 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -346 66 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -346 66 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -346 66 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
185 10778 60 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
44448063 162024 0 UNDEFINED 3 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
CHEMBL402736 162024 0 UNDEFINED 3 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
68617 212306 62 3H-SCH23390 -912 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 212306 62 3H-SCH23390 -912 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 212306 62 3H-SCH23390 -912 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
1242 10385 27 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1588 9105 27 3H-SCH23390 -131 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 3H-SCH23390 -131 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 3H-SCH23390 -131 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 3H-SCH23390 -131 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 3H-SCH23390 -131 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
10355510 162441 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL404865 162441 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
None 223509 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 325 3 2 4 3.6 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O None
1353 8692 93 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448061 101622 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
CHEMBL253736 101622 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
None 224146 0 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 3 2 3 5.7 CCCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5.Cl None
20840341 222956 0 3H-dopamine -75 4 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 451 5 1 3 6.2 C1CN(CCC1CCO)CCC=C2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F None
115237 62359 119 3H-SCH23390 -2511 54 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-SCH23390 -2511 54 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
31101 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
25058166 222739 0 3H-SCH23390 -144 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 -144 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
16362 9899 71 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
10660476 54147 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
CHEMBL154468 54147 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
134551 7146 27 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 7146 27 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 7146 27 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 7146 27 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135398745 9688 112 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
127708 119298 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 119298 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
228 7233 28 None -4 23 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None -4 23 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None -4 23 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None -4 23 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None -4 23 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
2448 106099 70 None -5 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 106099 70 None -5 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
1212 8443 50 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 8692 93 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
180 7189 56 None -109 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 None -109 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 None -109 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 None -109 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 None -109 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1588 9105 27 None -131 44 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 None -131 44 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 None -131 44 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 None -131 44 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 None -131 44 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2274 9947 58 None -16 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -16 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -16 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -16 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -16 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2726 7706 68 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
25058166 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1613 9127 53 None -5 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -5 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -5 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -5 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -5 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
228 7233 28 None -30 23 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None -30 23 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None -30 23 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None -30 23 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None -30 23 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
212 10578 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 10578 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 10578 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 10578 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 10578 47 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
135398737 7745 93 None -83 90 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -83 90 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -83 90 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -83 90 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -83 90 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
21302490 119582 32 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 119582 32 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 119582 32 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
115237 62359 119 None -74 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -74 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398745 9688 112 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
133 9274 52 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2726 7706 68 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
103 10925 61 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1212 8443 50 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 10104 118 None -346 66 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -346 66 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -346 66 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -346 66 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -346 66 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 10104 118 None -489 66 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -489 66 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -489 66 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -489 66 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -489 66 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3389 224490 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
1353 8692 93 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11976 7707 59 None -12 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 7707 59 None -12 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 7707 59 None -12 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 7707 59 None -12 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
5281878 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
6761 74574 19 None -5 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 74574 19 None -5 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
1353 8692 93 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
16351 109507 47 None -4 6 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL304902 109507 47 None -4 6 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2435 10362 83 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
37459 7533 13 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
127708 119298 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 119298 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
7153 104796 77 3H-SCH23390 -371 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-SCH23390 -371 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
103 10925 61 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2284 9956 33 3H-dopamine -3019 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 9956 33 3H-dopamine -3019 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 9956 33 3H-dopamine -3019 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 9956 33 3H-dopamine -3019 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 9956 33 3H-dopamine -3019 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2337 10030 77 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
25186023 194523 0 UNDEFINED -50118 4 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl None
CHEMBL495572 194523 0 UNDEFINED -50118 4 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl None
25058166 222739 0 UNDEFINED -144 26 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 UNDEFINED -144 26 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
44448067 162308 0 UNDEFINED - 1 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 None
CHEMBL404240 162308 0 UNDEFINED - 1 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 None
5281878 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2726 7706 68 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1241 106955 24 3H-SCH23390 -2 8 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL288090 106955 24 3H-SCH23390 -2 8 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL552611 106955 24 3H-SCH23390 -2 8 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
30137 9652 0 UNDEFINED -3981 9 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 9652 0 UNDEFINED -3981 9 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 9652 0 UNDEFINED -3981 9 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2726 7706 68 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
214 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-dopamine -891 30 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5567 49576 27 3H-dopamine -812 8 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 49576 27 3H-dopamine -812 8 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2389 10104 118 3H-SCH23390 -346 66 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -346 66 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -346 66 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -346 66 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -346 66 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 10577 58 3H-SCH23390 -309 54 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SCH23390 -309 54 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SCH23390 -309 54 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SCH23390 -309 54 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SCH23390 -309 54 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 223917 0 UNDEFINED -199 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 359 1 3 4 4.2 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O None
1353 8692 93 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223194 0 3H-SCH23390 -676 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
16362 9899 71 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2470 10425 50 3H-SCH23390 -31622 58 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -31622 58 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -31622 58 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -31622 58 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -31622 58 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
681 8247 72 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 223737 0 UNDEFINED 8 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 280 1 1 3 3.0 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)N None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2107 9829 50 None -5 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
4747 9829 50 None -5 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
9216 9829 50 None -5 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
CHEMBL251940 9829 50 None -5 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
DB01608 9829 50 None -5 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
25058166 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2865 10915 73 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
681 8247 72 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
228 7233 28 None -35 23 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None -35 23 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None -35 23 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None -35 23 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None -35 23 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
5281878 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
62865 8057 0 None -2 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 8057 0 None -2 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 8057 0 None -2 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 8057 0 None -2 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 8057 0 None -2 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
1153 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 8409 58 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
25058166 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1238 209953 24 None -5 16 Rat 8.1 pKi = 8.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 209953 24 None -5 16 Rat 8.1 pKi = 8.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
46780481 114308 20 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
37459 7533 13 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
15139 205859 52 3H-dopamine -794 5 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 356 7 0 4 3.6 COc1ccccc1N1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL58792 205859 52 3H-dopamine -794 5 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 356 7 0 4 3.6 COc1ccccc1N1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
16219195 222910 0 3H-dopamine 1 5 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 325 1 1 5 2.9 CN1CCC2=CC3=C(C4=C2C1CC5=C4C(=C(C=C5)OC)O)OCO3 None
None 223504 0 UNDEFINED - 1 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 325 4 0 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C(=CC=C4)OC=O None
5281878 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
180 7189 56 3H-SCH23390 -158 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 3H-SCH23390 -158 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 3H-SCH23390 -158 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 3H-SCH23390 -158 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 3H-SCH23390 -158 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1353 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
484 9633 51 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2780 117306 36 3H-SCH23390 -630 10 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 3H-SCH23390 -630 10 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
1353 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448064 101649 0 UNDEFINED 1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL253947 101649 0 UNDEFINED 1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
1353 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL146246 45052 0 3H-SCH23390 -2290 9 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 None
103 10925 61 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2470 10425 50 3H-SCH23390 -51286 58 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SCH23390 -51286 58 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SCH23390 -51286 58 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SCH23390 -51286 58 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SCH23390 -51286 58 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135398737 7745 93 3H-SCH23390 -83 90 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 8442 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 8442 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 8442 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
135398745 9688 112 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
44448060 162023 0 UNDEFINED -1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 None
CHEMBL402735 162023 0 UNDEFINED -1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 None
None 223912 0 UNDEFINED -269 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 116 4 0 2 1.4 CCCCN(C)N=O None
25058166 222739 0 3H-SCH23390 -147 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SCH23390 -147 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
135398737 7745 93 3H-SCH23390 -83 90 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SCH23390 -83 90 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SCH23390 -83 90 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SCH23390 -83 90 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SCH23390 -83 90 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44591012 182359 0 UNDEFINED -177 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL457957 182359 0 UNDEFINED -177 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
None 223916 0 UNDEFINED 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 343 1 2 3 4.5 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5 None
3168 16034 92 3H-dopamine -1318 22 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 3H-dopamine -1318 22 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
180 7189 56 UNDEFINED -109 40 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 UNDEFINED -109 40 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 UNDEFINED -109 40 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 UNDEFINED -109 40 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 UNDEFINED -109 40 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398737 7745 93 UNDEFINED -44 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -44 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -44 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -44 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -44 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 10577 58 3H-SCH23390 -47 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SCH23390 -47 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SCH23390 -47 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SCH23390 -47 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SCH23390 -47 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
681 8247 72 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
242 7258 124 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
37459 7533 13 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
2865 10915 73 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
6603820 102549 19 3H-SCH23390 1 12 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 1 12 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2726 7706 68 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
6852400 222716 0 3H-SCH23390 -22387 22 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-SCH23390 -22387 22 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
None 222914 0 3H-KETANSERIN -9332 23 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
5281878 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223510 0 UNDEFINED - 1 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 311 2 3 4 3.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)O)C(=C(C=C4)O)O None
24949535 188338 0 UNDEFINED -1122 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 None
CHEMBL476722 188338 0 UNDEFINED -1122 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 None
5074 10105 80 3H-SCH23390 -1621 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 3H-SCH23390 -1621 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 3H-SCH23390 -1621 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 3H-SCH23390 -1621 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 224147 0 UNDEFINED - 1 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 423 3 3 4 5.4 CCCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O.Cl None
2726 7706 68 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
5 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-SCH23390 -23442 53 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1242 10385 27 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 10385 27 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 10385 27 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
5281878 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
5281878 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
5281881 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
5281881 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
948 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
948 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
968 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
968 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
CHEMBL42055 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL42055 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
CHEMBL54661 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL54661 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
DB00875 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00875 8441 35 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
681 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
681 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
940 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
940 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
947 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
947 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
CHEMBL59 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
CHEMBL59 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
DB00988 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
DB00988 8247 72 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
5 6927 72 None -23442 53 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
5202 6927 72 None -23442 53 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
CHEMBL39 6927 72 None -23442 53 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
DB08839 6927 72 None -23442 53 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
1153 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026874 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026875 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1160786 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 8409 58 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
1242 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
1242 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
935 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
935 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
CHEMBL286080 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL286080 10385 27 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
1712 9270 43 None -6 22 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
4078 9270 43 None -6 22 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
7227 9270 43 None -6 22 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
CHEMBL1088 9270 43 None -6 22 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
DB00933 9270 43 None -6 22 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
2274 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -16 31 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1153 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
12668023 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
30026874 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
30026875 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
3341 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
6603851 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
933 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
939 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
985 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL1160786 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL1161520 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL588 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
DB00800 8409 58 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
1153 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026874 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026875 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1160786 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 8409 58 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
1353 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
1353 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
3559 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
3559 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
86 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
86 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
CHEMBL54 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
CHEMBL54 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
DB00502 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
DB00502 8692 93 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
5311070 8199 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
9267 8199 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
CHEMBL4280145 8199 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
DB12890 8199 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
2107 9829 50 None -5 2 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
4747 9829 50 None -5 2 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
9216 9829 50 None -5 2 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
CHEMBL251940 9829 50 None -5 2 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
DB01608 9829 50 None -5 2 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
13372 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 30525590
86764100 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 30525590
CHEMBL3697617 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 30525590
DB14899 10531 30 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 3 1 5 3.6 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C 30525590
107930 8311 26 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
3304 8311 26 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
CHEMBL298406 8311 26 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
DB12273 8311 26 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
5018 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
5018 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
943 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
943 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
946 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
946 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
CHEMBL13668 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
CHEMBL13668 10322 13 None 2 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
1218 10388 30 None 11 8 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
938 10388 30 None 11 8 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
CHEMBL353335 10388 30 None 11 8 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
6603703 6996 10 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
9637 6996 10 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
CHEMBL291143 6996 10 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
1243 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
944 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
CHEMBL324017 10390 34 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
2995 211184 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
5770 211837 82 None -2 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
CHEMBL772 211837 82 None -2 7 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
213 10625 55 None -12 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 None -12 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 None -12 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 None -12 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 None -12 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2601 10552 33 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
484 9633 51 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
951 9633 51 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
CHEMBL432 9633 51 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
2407 10145 76 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
59227 10145 76 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
941 10145 76 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
CHEMBL1303 10145 76 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
DB05271 10145 76 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
228 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
228 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
33 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
33 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
6005 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
6005 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
CHEMBL53 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
CHEMBL53 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
DB00714 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
DB00714 7233 28 None -35 23 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
3153 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
3153 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
932 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
932 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
CHEMBL26736 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
CHEMBL26736 7085 28 None -831 8 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
2105 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2105 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
47811 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
48 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
CHEMBL531 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
DB01186 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 9828 37 None -123 32 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
31101 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
31101 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
35 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
403 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
CHEMBL493 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
DB01200 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 7516 40 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
937 10387 0 None -1 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1826762
37 7565 60 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 7565 60 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 7565 60 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 7565 60 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 7565 60 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
1524 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
197 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
3822 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
88 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
CHEMBL51 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
DB12465 8962 96 None -79 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
2470 10425 50 None -4168 58 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
3300 10425 50 None -4168 58 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
5265 10425 50 None -4168 58 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
99 10425 50 None -4168 58 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
CHEMBL267930 10425 50 None -4168 58 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
135398737 7745 93 None -44 90 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
38 7745 93 None -44 90 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
722 7745 93 None -44 90 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
CHEMBL42 7745 93 None -44 90 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
DB00363 7745 93 None -44 90 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
100 10577 58 None -47 54 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
2637 10577 58 None -47 54 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
5452 10577 58 None -47 54 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
CHEMBL479 10577 58 None -47 54 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
DB00679 10577 58 None -47 54 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
2726 7706 68 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
621 7706 68 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
83 7706 68 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
CHEMBL71 7706 68 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
DB00477 7706 68 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
1588 9105 27 None -131 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 9105 27 None -131 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 9105 27 None -131 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 9105 27 None -131 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 9105 27 None -131 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
30137 9652 0 None -676 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
8594 9652 0 None -676 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
934 9652 0 None -676 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
37459 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
37459 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
62 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
62 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
CHEMBL8514 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
CHEMBL8514 7533 13 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
1212 8443 50 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
204 8443 50 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
3372 8443 50 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL726 8443 50 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00623 8443 50 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
173871 10386 2 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652
936 10386 2 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652
CHEMBL1193571 10386 2 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652