Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1153 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 3372 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 3372 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 3372 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 3372 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 3372 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 3081 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 3081 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 3081 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 3081 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 3081 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 788 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 788 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 788 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 788 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 788 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 3331 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 3331 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 3331 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 3331 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 3331 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 3054 37 None -85 25 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 3054 37 None -85 25 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 3054 37 None -85 25 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 3054 37 None -85 25 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 3054 37 None -85 25 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 1414 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 1414 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 1414 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 1414 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 1414 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 7072 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 7072 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 7072 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 78150 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 78150 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 958 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
38 958 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
722 958 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 958 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 958 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 1454 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 1454 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 1454 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 1454 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 1454 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 78221 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 78221 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
228 445 28 None -14 20 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
33 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 89130 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 89130 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 150698 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 150698 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 84686 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 84686 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 84370 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 84370 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 729 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
35 729 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
403 729 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 729 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 729 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 37294 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 37294 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 10798 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 10798 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 11848 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 11848 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 11848 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 11848 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 204626 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 204626 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 178619 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 178619 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 5258 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 5258 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 61560 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 61560 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 4127 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 4127 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 4127 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 4127 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 4127 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 33613 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 33613 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 597 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
333 597 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 597 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 597 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 597 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 597 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 3095 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 3095 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 3095 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 3095 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 3095 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 3991 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 3991 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 3991 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 3991 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 3991 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 1658 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 1658 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 1658 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 1658 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 1658 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 205097 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 205097 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 107531 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 107531 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 107531 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 107531 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 78243 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 78243 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 3330 96 None -2290 27 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 3330 96 None -2290 27 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 3330 96 None -2290 27 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 3330 96 None -2290 27 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 3330 96 None -2290 27 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 14493 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 14493 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 14493 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 14493 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 14493 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 14493 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 115564 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 115564 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 2509 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 2509 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 2509 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 2509 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 2509 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 2857 67 None -24 18 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 2857 67 None -24 18 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 2857 67 None -24 18 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 2857 67 None -24 18 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 2857 67 None -24 18 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 2385 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 2385 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 2385 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 2385 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 2385 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 3100 67 None -851 14 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 3100 67 None -851 14 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 3100 67 None -851 14 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 3100 67 None -851 14 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 3100 67 None -851 14 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 188966 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 291 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 291 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
479 291 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 291 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 291 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 291 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 2914 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 2914 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 2914 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 2914 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 3773 41 None -208 35 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 3773 41 None -208 35 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 3773 41 None -208 35 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 1420 21 None -1949 25 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 1420 21 None -1949 25 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 1420 21 None -1949 25 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 1420 21 None -1949 25 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 1420 21 None -1949 25 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
37 778 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
460 778 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 778 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 778 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 778 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 2540 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 2540 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 2540 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 2540 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 2540 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 4143 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 4143 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 4143 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 4143 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 4143 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 103112 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 103112 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 3860 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 3860 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 3860 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 3860 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 3860 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 3860 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 9157 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 9157 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 60080 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 60080 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 205818 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 205818 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 205818 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 3780 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 3780 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 3780 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 3780 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 3780 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
242 470 124 None -794 33 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
34 470 124 None -794 33 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 470 124 None -794 33 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 470 124 None -794 33 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 470 124 None -794 33 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 4153 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 4153 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 4153 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 4153 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 4153 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 52037 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 52037 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 1582 14 None -5011 22 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 1582 14 None -5011 22 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 1582 14 None -5011 22 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 1582 14 None -5011 22 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 1582 14 None -5011 22 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 1911 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 1911 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 1911 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 1911 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 1911 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 3134 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 3134 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 3134 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 3134 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 3134 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 3256 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 3256 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 3256 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 3256 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 3256 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 2617 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 2617 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 2617 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 596 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
312 596 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 596 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 596 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 596 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 2590 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 2590 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 2590 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 2590 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 2590 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 3806 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 3806 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 3806 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 3806 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 3806 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 13889 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 13889 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 13889 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 3619 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 3619 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 3619 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 171611 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 171611 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 171611 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 171611 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 166425 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 166425 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 166425 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 166425 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 170810 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 170810 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 172060 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 172060 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 170810 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 170810 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 3614 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 3614 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 3614 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 16257 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 16257 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 3617 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 3617 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 3617 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 171727 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 171727 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 171727 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 171727 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 100179 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 100179 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 100179 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 161887 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 161887 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 2876 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 2876 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 2876 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 2876 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 2876 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 2876 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 3613 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 3613 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 3613 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 2524 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 2524 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 2524 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 169282 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 169282 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 169282 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 169630 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 169630 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 169630 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 169630 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 170571 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 170571 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 170571 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 170571 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 107067 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 107067 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 175270 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 175270 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 106831 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 106831 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 175270 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 175270 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 176196 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 176196 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 176196 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 176196 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 205 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 205 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 205 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 205 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 205 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 205 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 205 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 205 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 205 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 174206 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 174206 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 171916 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 171916 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 102480 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 102480 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 102480 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 120480 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 120480 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 171107 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 171107 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 206313 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 206313 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 11554 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 11554 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 11554 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 169703 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 169703 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 4440 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 4440 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 168205 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 168205 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 169703 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 169703 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 171107 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 171107 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 166425 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 166425 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 192200 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 192200 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 171709 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 171709 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 160640 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 160640 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 87572 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 87572 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 166425 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 166425 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 171709 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 171709 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 98389 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 98389 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 82161 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 82161 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 82161 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 141411 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 141411 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 174581 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 174581 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 166732 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 166732 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 170515 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 170515 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 120480 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 120480 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 167073 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 167073 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 174581 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 174581 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 102472 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 102472 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 102472 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 180719 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 180719 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 172242 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 172242 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 172242 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 172242 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 163967 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 163967 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 176084 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 176084 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 106268 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 106268 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 106268 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 173965 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 173965 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 99740 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 99740 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 180610 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 180610 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 166897 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 166897 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 20979 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 20979 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 173965 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 173965 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 167279 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 167279 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 206228 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 206228 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 100163 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 100163 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 48520 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 48520 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 191116 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 191116 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 176031 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 176031 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 191084 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 191084 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 176084 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 176084 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 171519 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 171519 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 164108 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 164108 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 118814 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 118814 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 3613 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 3613 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 3613 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 175351 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 175351 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 190462 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 190462 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 175351 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 175351 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 166893 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 166893 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 172585 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 172585 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 180692 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 180692 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 95774 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 95774 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 175483 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 175483 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 100386 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 100386 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 171267 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 171267 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 166425 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 166425 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 171267 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 171267 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 79666 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 79666 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 175483 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 175483 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 130709 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 130709 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 130709 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 172348 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 172348 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 104266 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 104266 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 106283 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 106283 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 106283 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 181035 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 181035 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 181922 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 181922 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 175587 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 175587 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 175587 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 175587 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 166514 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 166514 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 169671 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 169671 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 169671 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 169671 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 173222 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 173222 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 173222 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 173222 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 182682 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 182682 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 192225 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 192225 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 37686 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 37686 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 172348 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 172348 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 205773 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 205773 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 2412 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 2412 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 2412 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 13228 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 13228 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 13228 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 175193 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 175193 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 118814 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 118814 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 175193 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 175193 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 181301 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 181301 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 183248 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 183248 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 179749 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 179749 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 166425 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 166425 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 142015 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 142015 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 147014 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 147014 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 3613 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 3613 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 3613 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 179428 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 179428 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 175316 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 175316 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 206079 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 206079 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 100433 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 100433 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 100433 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 97628 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 97628 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 173751 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 173751 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 206016 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 206016 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 3613 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 3613 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 3613 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 174159 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 174159 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 99494 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 99494 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 174159 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 174159 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 179459 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 179459 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 182813 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 182813 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 192510 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 192510 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 95774 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 95774 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 106286 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 106286 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 106286 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 172264 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 172264 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 175652 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 175652 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 175652 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 175652 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 172264 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 172264 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 180625 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 180625 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 181453 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 181453 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 10239 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 10239 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 106032 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 106032 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 107029 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 107029 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 205 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 205 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 205 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 171685 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 171685 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 171685 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 171685 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 171908 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 171908 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 171908 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 171908 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 2524 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 2524 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 2524 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 167337 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 167337 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 167337 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 167337 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 171916 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 171916 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 111468 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 111468 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 111468 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 111468 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 199066 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 199066 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 174029 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 174029 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 102475 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 102475 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 102475 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 104263 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 104263 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 173044 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 173044 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 190320 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 190320 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 191494 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 191494 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 84412 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 84412 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 84412 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 174029 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 174029 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 170405 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 170405 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 166685 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 166685 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 3691 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 3691 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 3691 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 97665 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 97665 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 164108 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 164108 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 104267 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 104267 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 99316 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 99316 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 191512 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 191512 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 79559 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 79559 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 182773 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 182773 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 206424 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 206424 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 171761 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 171761 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 171761 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 171761 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 84411 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 84411 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 84411 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 99519 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 99519 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 206212 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 206212 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 13781 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 13781 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 13781 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 166853 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 166853 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 183281 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 183281 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 155732 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 155732 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 100179 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 100179 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 100179 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
228 445 28 None -14 20 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
33 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 173044 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 173044 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 166685 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 166685 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 166685 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 166685 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 180799 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 180799 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 170298 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 170298 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 170298 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 170298 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 167337 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 167337 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 171968 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 171968 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 171968 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 171968 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 146578 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 146578 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 146578 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 146578 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 107035 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 107035 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 179445 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 179445 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 100507 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 100507 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 156415 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 156415 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 3372 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 3372 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 3372 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 3372 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 3372 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 170514 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 170514 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 174710 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 174710 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 171469 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 171469 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 141958 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 141958 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 60025 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 60025 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 181073 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 181073 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 2524 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 2524 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 2524 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 106831 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 106831 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 206399 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 206399 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 118815 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 118815 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
228 445 28 None -14 20 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
33 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 16258 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 16258 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
228 445 28 None -14 20 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
33 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 91599 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 91599 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 91599 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 91599 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 95774 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 95774 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 174529 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 174529 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 163424 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 163424 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 3613 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 3613 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 3613 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 191075 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 191075 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 101363 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 101363 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 101363 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 174527 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 174527 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 174527 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 174527 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 118814 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 118814 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 102460 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 102460 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 102460 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 173524 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 173524 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 82406 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 82406 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 173524 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 173524 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 99078 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 99078 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 13259 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 13259 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 13259 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 84413 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 84413 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 84413 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 166425 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 166425 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 106285 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 106285 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 106285 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 170405 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 170405 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 169762 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 169762 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 206426 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 206426 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 171624 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 171624 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 169762 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 169762 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 171624 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 171624 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 104264 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 104264 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 172312 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 172312 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 107041 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 107041 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 99702 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 99702 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 172779 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 172779 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 91599 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 91599 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 91599 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 91599 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 3613 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 3613 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 3613 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 172779 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 172779 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 100229 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 100229 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 206212 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 206212 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 104265 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 104265 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 16252 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 16252 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 3616 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 3616 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 3616 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 104268 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 104268 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 12972 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 12972 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 12972 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 13090 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 13090 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 13090 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 170531 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 170531 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 3691 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 3691 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 3691 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 166514 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 166514 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 182305 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 182305 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 100473 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 100473 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 182318 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 182318 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 182563 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 182563 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 66494 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 66494 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 66494 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 100377 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 100377 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 1465 72 None -77 15 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 172855 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 172855 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 173813 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 173813 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 163424 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 163424 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 174660 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 174660 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 98774 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 98774 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 158866 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 158866 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 163173 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 163173 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 206432 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 206432 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 208344 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 208344 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 208344 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 107366 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 107366 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 192006 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 192006 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 87571 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 87571 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 106141 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 106141 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 208 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 208 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 208 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 206016 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 206016 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 132437 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 132437 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 71539 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 71539 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 71539 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 169799 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 169799 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 169799 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 169799 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 206099 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 206099 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 118814 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 118814 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 169933 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 169933 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 11560 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 11560 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 11560 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 1465 72 None -1380 15 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 169978 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 169978 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 169978 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 169978 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 146578 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 146578 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 146578 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 146578 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
228 445 28 None -14 20 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
33 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 445 28 None -14 20 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 205773 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 205773 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 172948 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 172948 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 172948 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 172948 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 175372 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 175372 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 171610 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 171610 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 166953 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 166953 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 175372 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 175372 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 181114 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 181114 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 91599 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 91599 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 91599 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 91599 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 174529 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 174529 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 66600 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 66600 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 66600 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 174930 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 174930 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 66502 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 66502 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 66502 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 167894 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 167894 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 106963 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 106963 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 206063 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 206063 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 99277 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 99277 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 3910 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 3910 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 3910 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 170487 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 170487 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 170116 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 170116 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 170487 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 170487 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 171973 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 171973 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 170116 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 170116 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 2524 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 2524 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 2524 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 100109 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 100109 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 166532 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 166532 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 162302 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 162302 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 171207 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 171207 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 171207 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 171207 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 205965 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 205965 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 170767 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 170767 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 169577 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 169577 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 3613 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 3613 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 3613 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 169577 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 169577 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 170767 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 170767 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 107083 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 107083 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 163799 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 163799 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 100433 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 100433 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 100433 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 107029 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 107029 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 95774 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 95774 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 176013 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 176013 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 176013 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 176013 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 157117 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 157117 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 171951 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 171951 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 171951 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 171951 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 106284 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 106284 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 106284 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 102473 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 102473 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 102473 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 171083 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 171083 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 87281 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 87281 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 118815 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 118815 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 162755 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 162755 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 171083 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 171083 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 171549 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 171549 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 171549 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 171549 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 102467 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 102467 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 102467 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 161255 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 161255 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 173032 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 173032 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 173032 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 173032 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 87575 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 87575 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 208 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 208 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 208 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 106141 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 106141 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 97376 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 97376 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 99880 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 99880 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 168474 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 168474 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 96648 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 96648 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 169630 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 169630 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 171526 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 171526 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 11226 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 11226 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 11226 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 167315 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 167315 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 174505 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 174505 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 174505 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 180761 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 180761 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 205787 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 205787 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 205787 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 205787 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 100310 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 100310 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 100310 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 176017 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 176017 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 176017 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 176017 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 95774 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 95774 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 100265 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 100265 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 170614 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 170614 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 104262 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 104262 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 206175 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 206175 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 170614 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 170614 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 167296 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 167296 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 99519 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 99519 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 100409 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 100409 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 91599 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 91599 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 91599 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 91599 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 174684 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 174684 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 173791 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 173791 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 173791 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 173791 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 1529 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 1529 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 1529 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 1529 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 202754 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 202754 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 202754 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 202754 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 175718 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 175718 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 86479 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 86479 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 83528 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 83528 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 76068 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 76068 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 202045 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 202045 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 202474 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 202474 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 202474 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 76073 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 76073 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 172382 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 172382 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 171761 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 171761 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 1911 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 1911 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 1911 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 1911 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 1911 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 186118 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 186118 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 197556 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 197556 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 37686 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 37686 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 198136 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 198136 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 115189 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 115189 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 172585 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 172585 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 76067 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 76067 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 101705 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 101705 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 100633 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 100633 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 197719 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 197719 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 194943 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 194943 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 196778 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 196778 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 198744 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 198744 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 167314 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 167314 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
228 445 28 None -131 20 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
33 445 28 None -131 20 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 445 28 None -131 20 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 445 28 None -131 20 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 445 28 None -131 20 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 174891 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 174891 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 174891 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 174891 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 169735 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 169735 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 86481 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 86481 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 202474 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 202474 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 202474 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 175587 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 175587 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 175587 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 175587 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 202754 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 202754 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 202754 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 202754 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 1911 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 1911 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 1911 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 1911 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 1911 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 202754 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 115188 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 115188 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 3549 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 3549 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 3549 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 3549 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 86482 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 86482 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 174774 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 174774 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 173150 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 173150 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 172779 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 172779 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 174059 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 174059 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 172779 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 172779 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 197252 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 197252 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 169779 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 169779 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 169779 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 169779 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 177777 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 177777 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 75173 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 75173 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 3619 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 3619 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 3619 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 73152 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 73152 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 73152 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 74699 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 74699 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 73386 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 73386 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 141215 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 141215 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 9879 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 9879 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 3613 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 3613 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 3613 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 140882 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 140882 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 81581 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 81581 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 74694 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 74694 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 74694 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 75422 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 75422 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 73087 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 73087 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 7554 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 7554 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 140165 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 140165 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 75416 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 75416 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 48469 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 48469 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 140842 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 140842 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 141323 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 141323 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 81833 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 81833 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 75291 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 75291 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 184853 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 184853 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 139555 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 139555 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 180153 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 180153 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 73395 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 73395 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 958 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
38 958 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
722 958 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 958 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 958 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 140848 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 140848 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 185714 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 185714 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 140188 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 140188 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 73152 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 73152 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 73152 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 169313 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 169313 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 169313 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 169313 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 75252 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 75252 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 73408 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 73408 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 2035 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 2035 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 2035 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 185876 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 185876 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 186231 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 186231 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 1471 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 1471 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 1471 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 1471 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 1471 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 3619 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 3619 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 3619 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 3910 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 3910 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 3910 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 2524 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 2524 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 2524 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 2524 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 2524 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 2524 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 205 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 205 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 205 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 2412 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 2412 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 2412 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 3805 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 3805 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 3805 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 3805 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 3805 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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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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3294 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 4153 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 4153 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 4153 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 4153 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 4153 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 107531 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 107531 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 107531 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 107531 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 7072 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 7072 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 7072 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 188966 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 86804 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 86804 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 3162 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 3162 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 3162 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 3162 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 3162 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 175669 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 175669 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 175669 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 175669 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 2348 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 2348 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 2348 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 2348 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 2348 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 114692 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 114692 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 114692 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 195522 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 195522 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 3607 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 3607 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 3607 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 3607 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 3607 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 3182 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 3182 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 3182 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 3182 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 3182 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 2590 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 2590 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 2590 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 2590 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 2590 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 204008 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 204008 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 204008 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 4143 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 4143 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 4143 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 4143 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 4143 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 155656 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 155656 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 4530 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 4530 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 78207 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 78207 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 167976 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 167976 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 167976 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2385 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 2385 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 2385 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 2385 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 2385 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 4097 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 4097 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 4097 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 4097 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 4097 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 61061 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 61061 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 204865 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 204865 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 204865 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 204865 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 1576 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 1576 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 1576 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 1576 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 1576 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 1433 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 1433 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 1433 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 1433 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 1433 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3256 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 3256 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 3256 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 3256 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 3256 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 100404 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 100404 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 3860 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 3860 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 3860 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 3860 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 3860 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 3860 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 133512 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 133512 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 133512 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 78210 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 78210 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 202133 58 None - 5 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 202133 58 None - 5 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 2385 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 2385 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 2385 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 2385 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 2385 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 205639 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 205639 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 205639 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 344 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 344 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 344 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 344 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 344 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 949 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 949 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
671 949 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 949 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 949 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 169420 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 169420 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 2914 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 2914 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 2914 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 2914 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 954 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 954 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
701 954 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 954 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 954 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 35922 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 35922 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 1280 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 1280 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 1280 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 1280 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 1280 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 14487 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 14487 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 203211 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 203211 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 120519 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 120519 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 3817 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 3817 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 3817 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 3817 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 3817 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 5258 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 5258 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 1657 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 1657 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 1657 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 1657 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 110035 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 110035 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 78294 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 78294 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 203488 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 203488 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 188796 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 188796 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 188796 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 2514 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 2514 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 2514 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 2514 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 2514 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 2759 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 2759 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 2759 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 2759 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 2759 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 57405 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 57405 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 101562 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 101562 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 3703 110 None -549 21 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 41514 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 41514 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 188966 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 197500 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 197500 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 197500 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 197500 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 84539 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 84539 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 3183 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 3183 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 3183 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 3183 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 3183 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 15299 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 15299 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 15299 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 3100 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 3100 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 3100 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 3100 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 3100 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 205552 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 205552 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
191 403 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
201 403 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 403 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 403 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 403 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 2822 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 2822 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 2822 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 2822 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 2822 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 2822 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 3806 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 3806 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 3806 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 3806 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 3806 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 11848 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 11848 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 11848 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 11848 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 78151 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 78151 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 4153 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 4153 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 4153 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 4153 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 4153 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 14503 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 14503 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 3863 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 3863 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 3863 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 3863 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 3863 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 13044 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 13044 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 56130 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 56130 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 56130 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 3129 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 3129 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 3129 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 3129 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 78409 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 78409 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 140606 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 140606 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 940 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
654 940 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 940 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 940 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 940 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 14500 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 14500 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 46035 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 46035 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 34222 85 None - 6 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 34222 85 None - 6 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 198318 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 198318 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 102400 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 102400 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 166911 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 166911 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 166911 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 95001 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 95001 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 95001 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 206747 35 None - 16 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 206747 35 None - 16 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 206747 35 None - 16 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 4127 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 4127 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 4127 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 4127 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 4127 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 13620 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 13620 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 133512 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 133512 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 133512 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 176149 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 176149 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 176149 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 176149 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 803 103 None -112 21 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
522 803 103 None -112 21 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
551 803 103 None -112 21 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 803 103 None -112 21 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 803 103 None -112 21 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 207841 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 207841 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 2341 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 2341 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 2341 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 2341 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 2341 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 204995 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 204995 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 55562 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 55562 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 55562 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 214034 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 729 40 None -436 36 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
35 729 40 None -436 36 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
403 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 2348 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 2348 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 2348 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 2348 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 2348 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 44129 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 44129 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 5436 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 5436 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 80483 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 80483 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 2489 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 2489 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 2489 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 2489 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 2489 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 2489 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 1651 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 1651 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 1651 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 1651 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 1651 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 150698 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 150698 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 19077 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 19077 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 20333 57 None -12 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 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 20333 57 None -12 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 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 60504 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 60504 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 3128 46 None - 35 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 3128 46 None - 35 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 3128 46 None - 35 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 3128 46 None - 35 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 3128 46 None - 35 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 194536 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 32505 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 32505 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 32505 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 69379 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 69379 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 882 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 882 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
583 882 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 882 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 882 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 107081 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 107081 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 1547 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 1547 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 1547 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 1547 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 1547 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 19221 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 19221 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 3777 64 None - 13 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 3777 64 None - 13 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 3777 64 None - 13 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 3777 64 None - 13 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 3777 64 None - 13 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 56267 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 56267 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 3162 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 3162 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 3162 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 3162 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 3162 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 78151 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 78151 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 167519 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 167519 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 3779 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 3779 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 3779 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 3779 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 3779 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 9812 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 9812 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 14478 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 14478 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 39794 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 39794 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 800 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 800 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 800 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 800 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 800 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 800 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 920 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 920 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 920 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 920 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 4143 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 4143 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 4143 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 4143 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 4143 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 214033 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 56267 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 56267 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 1301 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 1301 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 1301 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 1301 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 1301 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 2013 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 2013 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 2013 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 2013 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 2013 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 45822 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 45822 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 3183 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 3183 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 3183 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 3183 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 3183 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 1389 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 1389 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 1389 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 1389 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 1389 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 167519 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 167519 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 94792 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 94792 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 11848 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 11848 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 11848 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 11848 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 139067 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 139067 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 78206 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 78206 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 2866 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 2866 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 2866 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 2866 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 2866 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 195017 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 195017 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 195017 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 28085 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 28085 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 4143 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 4143 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 4143 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 4143 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 4143 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 3780 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 3780 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 3780 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 3780 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 3780 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 17961 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 17961 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 70460 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 70460 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 88581 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 88581 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 88581 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 1662 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 1662 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 1662 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 1662 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 1662 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 78221 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 78221 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 2325 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 2325 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 2325 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 2325 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 2325 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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
180 401 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
200 401 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 401 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 401 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 401 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 103793 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 103793 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1470 71 None - 10 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 1470 71 None - 10 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 1470 71 None - 10 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 1470 71 None - 10 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 1470 71 None - 10 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 100216 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 100216 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 60403 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 60403 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 194726 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 194726 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 102888 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 102888 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 102888 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 3125 71 None -52480 30 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 3125 71 None -52480 30 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 3125 71 None -52480 30 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 3125 71 None -52480 30 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 3125 71 None -52480 30 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 94791 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 94791 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 14465 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 14465 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 3056 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 3056 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 3056 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 3056 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 3056 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 66199 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 66199 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 1590 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 1590 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 1590 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 1590 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 1590 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 3256 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 3256 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 3256 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 3256 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 3256 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 919 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
621 919 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
83 919 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 919 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 919 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 160250 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 160250 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 45032 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 45032 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 3372 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 3372 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 3372 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 3372 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 3372 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 78294 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 78294 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 140606 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 140606 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 70460 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 70460 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 3124 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 3124 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 3124 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 3124 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 3124 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 78248 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 78248 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 161890 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 161890 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 60297 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 60297 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 102730 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 102730 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 3287 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 3287 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 3287 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 3287 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 3287 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 3287 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 98869 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 98869 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 187821 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 187821 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
37 778 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
460 778 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 778 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 778 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 778 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 84246 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 84246 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 17986 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 17986 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 17986 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 150698 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 150698 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 84308 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 84308 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 60283 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 60283 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 46950 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 46950 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 3055 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 3055 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 3055 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 3055 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 3055 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 28724 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 28724 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 56344 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 56344 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 2492 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 2492 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 2492 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 2492 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 2492 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 195017 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 195017 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 195017 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 3773 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 3773 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 3773 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 154653 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 154653 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 41658 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 41658 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 2914 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 2914 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 2914 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 2914 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 3806 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 3806 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 3806 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 3806 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 3806 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 1888 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 1888 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 1888 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 1888 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 1888 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 1888 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 28618 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 28618 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 28618 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 28618 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 28618 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 3256 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 3256 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 3256 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 3256 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 3256 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 1658 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 1658 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 1658 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 1658 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 1658 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 157531 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 157531 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 48449 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 48449 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 3163 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 3163 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 3163 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 3163 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 3163 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 3163 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 205134 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 205134 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 78187 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 78187 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 56343 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 78141 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 78141 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 3779 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 3779 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 3779 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 3779 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 3779 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
180 401 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
200 401 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 401 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 401 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 401 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 78395 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 78395 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 16649 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 16649 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 16649 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 3773 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 3773 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 3773 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 14005 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 14005 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 150108 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 150108 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 195115 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 195115 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 195115 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 55822 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 55822 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 505 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
249 505 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 505 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 505 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 505 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 169671 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 169671 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 169671 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 169671 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 176017 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 176017 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 176017 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 176017 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 174710 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 174710 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 91599 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 91599 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 91599 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 91599 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 2412 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 2412 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 2412 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 166425 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 166425 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 176084 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 176084 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 169630 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 169630 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 176084 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 176084 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 166425 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 166425 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 180799 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 180799 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 10239 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 10239 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 95774 19 None -4 13 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 95774 19 None -4 13 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 173222 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 173222 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 179445 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 179445 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 175316 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 175316 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 180610 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 180610 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 180761 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 180761 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 182563 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 182563 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 183281 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 183281 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 2412 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 2412 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 2412 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 179749 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 179749 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 180625 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 180625 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 173076 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 173076 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 146578 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 146578 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 146578 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 146578 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 167337 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 167337 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 167337 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 167337 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 181114 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 181114 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 181073 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 181073 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 2876 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 2876 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 2876 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 171600 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 171600 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 2876 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 2876 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 2876 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 171951 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 171951 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 171951 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 171951 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 3617 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 3617 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 3617 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 13889 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 13889 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 13889 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 181035 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 181035 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 170571 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 170571 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 171611 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 171611 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 170571 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 170571 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 171611 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 171611 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 175270 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 175270 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 175270 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 175270 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 169978 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 169978 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 191112 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 191112 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 169978 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 169978 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 169799 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 169799 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 169799 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 169799 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 171908 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 171908 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 171908 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 171908 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 208 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 208 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 208 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 166425 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 166425 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 20979 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 20979 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 180692 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 180692 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 182318 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 182318 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 170810 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 170810 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 169779 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 169779 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 3616 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 3616 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 3616 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 169779 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 169779 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 182813 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 182813 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 181922 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 181922 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 100698 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 100698 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 100698 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 169577 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 169577 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 169577 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 169577 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 179459 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 179459 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 171916 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 171916 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 174527 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 174527 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 181301 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 181301 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 182773 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 182773 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 174527 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 174527 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 180719 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 180719 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 91599 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 91599 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 91599 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 91599 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 171519 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 171519 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 182305 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 182305 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 179428 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 179428 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 171727 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 171727 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 171727 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 171727 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 176075 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 176075 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 174206 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 174206 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 174206 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 174206 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 176075 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 176075 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 182682 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 182682 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 181453 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 181453 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 183248 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 183248 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 99519 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 99519 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 3616 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 3616 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 3616 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 161567 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 161567 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 26679 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 26679 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 26767 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 26767 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 27191 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 27191 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 26731 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 26731 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 26721 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 26721 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 26767 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 26767 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 119207 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 119207 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 119296 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 119296 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 26731 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 26731 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 119330 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 119330 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 119296 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 119296 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 26856 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 26856 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 27425 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 27425 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 27248 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 27248 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 27572 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 27572 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 28904 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 28904 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 203324 9 None -3 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 203324 9 None -3 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 203324 9 None -3 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 203324 9 None -3 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 97126 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 97126 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 97126 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 27191 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 27191 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 119207 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 119207 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 119179 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 119179 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 28904 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 28904 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 27363 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 27363 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 27425 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 27425 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 109169 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 109169 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 109169 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 174891 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 174891 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 204645 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 204645 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 173266 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 173266 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 173267 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 173267 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 12997 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 12997 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 12997 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 13238 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 13238 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 13238 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 98547 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 98547 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 98547 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 112356 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 112356 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 207319 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 207319 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 11249 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 11249 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 11249 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 98702 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 98702 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 98993 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 98993 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 99085 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 99085 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 99085 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 99559 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 99559 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 99736 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 99736 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 162499 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 162499 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 28355 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 28355 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 99559 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 99559 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 145155 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 145155 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 153775 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 153775 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 9756 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 9756 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 12691 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 12691 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 12691 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 145219 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 145219 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 13652 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 13652 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 99714 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 99714 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 2509 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 2509 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 2509 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 2509 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 2509 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 13384 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 13384 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 13384 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 9262 92 None -89 21 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 9262 92 None -89 21 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 161917 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 161917 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 161917 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 161917 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 95774 19 None 1 13 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 95774 19 None 1 13 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 13652 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 13652 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 174891 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 174891 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 27248 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 27248 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 13053 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 13053 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 13053 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 12442 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 12442 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 12442 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 954 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 954 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
701 954 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 954 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 954 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 205745 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 205745 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 111016 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 111016 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 13137 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 13137 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 13137 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 76065 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 76065 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 76064 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 76064 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 23814 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 23814 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 13143 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 13143 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 13143 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 9367 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 9367 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 200945 22 None -144 19 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 200945 22 None -144 19 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 200945 22 None -144 19 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 188949 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 188949 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 102858 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 102858 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 103110 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 103110 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 107401 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 107401 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 95774 19 None 1 13 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 95774 19 None 1 13 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 157117 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 157117 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 22220 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 22220 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 59400 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 59400 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 2063 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 2063 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 2063 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 2063 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 2063 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 2063 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 48215 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 48215 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 33935 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 33935 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 95648 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 95648 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 198864 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 198864 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 29825 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 29825 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 119406 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 119406 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 145896 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 145896 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 207890 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 207890 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 207890 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 5302 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 5302 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 5302 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 5302 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 204577 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 204577 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 142251 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 142251 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 47659 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 47659 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 43151 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 43151 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 163042 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 163042 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 76067 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 76067 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 87505 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 87505 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 76073 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 76073 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 76066 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 76066 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 76066 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 76066 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 176017 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 176017 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 29150 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 29150 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 176017 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 176017 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 68665 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 68665 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 175587 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 175587 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 95774 19 None 1 13 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 95774 19 None 1 13 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 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
71474024 144468 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 144468 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 28904 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 28904 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 169978 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 169978 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 169978 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 169978 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 176880 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 176880 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 949 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 949 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
671 949 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 949 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 949 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 12440 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 12440 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 12440 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 3173 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 3173 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 3173 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 3173 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 3173 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 138121 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 138121 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 1301 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 1301 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 1301 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 1301 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 1301 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 169779 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 169779 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 27106 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 27106 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 27115 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 27115 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 169779 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 169779 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 188271 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 188271 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 111326 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 111326 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 13394 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 13394 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 13394 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 28287 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 28287 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 48801 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 48801 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
240 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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
660 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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 48801 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 48801 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 100180 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 100180 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 100180 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 100180 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 100180 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 100180 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 95596 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 95596 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 2325 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 2325 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 2325 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 2325 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 2325 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 207192 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 207192 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 207192 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 13838 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 13838 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 13838 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 48739 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 48739 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 76064 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 76064 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 99956 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 99956 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 13569 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 13569 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 13569 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 119090 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 119090 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 207717 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 207717 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 100179 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 100179 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 100179 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 3613 27 None 1 18 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 3613 27 None 1 18 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 3613 27 None 1 18 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 97313 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 97313 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 116472 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 116472 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 145327 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 145327 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 161668 10 None - 5 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 161668 10 None - 5 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 204061 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 204061 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 27248 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 27248 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 31328 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 31328 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 115495 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 115495 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 98947 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 98947 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 919 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
621 919 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
83 919 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 919 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 919 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 102280 4 None -8 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 102280 4 None -8 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 102280 4 None -8 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 102280 4 None -8 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 203174 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 203174 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 102280 4 None -8 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 102280 4 None -8 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 119332 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 119332 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 27292 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 27292 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 3549 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 3549 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 3549 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 3549 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 27216 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 27216 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 204114 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 204114 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 207248 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 207248 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 10166 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 10166 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 10166 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 11253 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 11253 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 11253 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 96097 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 96097 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 96097 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 98987 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 98987 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 98987 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 99083 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 99083 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 99083 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 99426 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 99426 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 99426 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 10166 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 10166 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 10166 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 88544 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 88544 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 207006 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 207006 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 143247 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 143247 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 102284 1 None - 5 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 102284 1 None - 5 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 40039 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 40039 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 142331 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 142331 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 204435 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 204435 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 206974 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 206974 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 27451 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 27451 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 103043 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 103043 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 207841 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 207841 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 205976 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 205976 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 25129 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 25129 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 149767 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 149767 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 204160 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 204160 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 26315 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 26315 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 9623 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 9623 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 919 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
621 919 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
83 919 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 919 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 919 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 18000 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 18000 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 108352 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 108352 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 1662 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 1662 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 1662 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 1662 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 1662 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 172779 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 172779 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 9623 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 9623 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 164909 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 164909 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 194885 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 194885 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 95300 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 95300 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 13696 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 13696 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 13696 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 3182 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 3182 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 3182 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 3182 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 3182 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 27292 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 27292 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 186265 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 186265 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 9888 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 9888 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 18555 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 18555 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 172779 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 172779 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 13691 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 13691 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 13691 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 20333 57 None -12 16 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 20333 57 None -12 16 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 3779 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 3779 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 3779 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 3779 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 3779 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 164857 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 164857 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 745 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
36 745 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
437 745 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 745 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 745 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 9930 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 9930 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 3183 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 3183 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 3183 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 3183 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 3183 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 11028 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 11028 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 29085 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 29085 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 67239 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 67239 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 11384 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 11384 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 103110 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 103110 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 99910 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 99910 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 206119 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 206119 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 729 40 None -436 36 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
35 729 40 None -436 36 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
403 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 108601 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 108601 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 67798 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 67798 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 76070 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 76070 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 76070 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 76070 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 100671 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 100671 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 29616 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 29616 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 43151 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 43151 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 144072 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 144072 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 27292 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 27292 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 95229 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 95229 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 28441 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 28441 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 76074 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 76074 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 9494 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 9494 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 33297 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 33297 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 11245 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 11245 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 11245 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 12042 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 12042 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 12042 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 13731 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 13731 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 13731 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 96097 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 96097 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 96097 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 103773 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 103773 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 5349 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 5349 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 13204 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 13204 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 13204 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 176149 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 176149 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 176149 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 176149 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 26847 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 26847 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 67799 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 67799 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 154810 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 154810 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 203859 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 203859 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 76063 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 76063 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 76063 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 76063 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 11164 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 11164 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 189343 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 189343 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 16791 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 16791 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 194683 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 194683 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 9881 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 9881 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 172654 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 172654 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 172654 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 194683 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 194683 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 119540 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 119540 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 30445 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 30445 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 98116 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 98116 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 9611 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 9611 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 91599 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 91599 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 91599 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 91599 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 24989 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 24989 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
180 401 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
200 401 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 401 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 401 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 401 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 95595 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 95595 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 162214 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 162214 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 27509 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 27509 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 147160 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 147160 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 82408 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 82408 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 10466 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 10466 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 27013 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 27013 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 12915 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 12915 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 12915 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 28374 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 28374 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 28619 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 28619 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 115207 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 115207 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 3286 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 3286 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 3286 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 3286 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 3286 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 1657 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 1657 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 1657 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 1657 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 116749 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 116749 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 177918 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 177918 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 177918 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
191 403 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
201 403 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 403 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 403 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 403 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 10166 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 10166 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 10166 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 118275 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 118275 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 26999 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 26999 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 76073 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 76073 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 95740 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 95740 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 142129 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 142129 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 142129 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 142129 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 14541 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 14541 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 10166 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 10166 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 10166 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 11245 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 11245 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 11245 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 97140 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 97140 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 97140 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 99490 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 99490 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 99490 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 165417 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 165417 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 165417 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 193324 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 193324 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 10166 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 10166 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 10166 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 505 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
249 505 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 505 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 505 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 505 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 358 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
271 358 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
885 358 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 358 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 171761 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 171761 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 171761 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 171761 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 17986 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 17986 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 17986 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 31639 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 31639 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 143264 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 143264 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 3256 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 3256 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 3256 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 3256 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 3256 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 203607 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 203607 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 29718 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 29718 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 119207 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 119207 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 97495 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 97495 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 111591 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 111591 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 30108 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 30108 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 76068 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 76068 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 59284 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 59284 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 208600 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 31343 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 31343 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 143379 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 143379 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 119284 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 119284 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 95594 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 95594 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 143379 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 143379 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 154299 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 154299 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 198925 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 198925 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 119250 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 119250 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 3617 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 3617 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 3617 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 103110 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 103110 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 95774 19 None 1 13 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 95774 19 None 1 13 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 31155 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 31155 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 91599 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 91599 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 91599 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 91599 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 30238 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 30238 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 118748 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 118748 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 11245 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 11245 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 11245 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 99085 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 99085 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 99085 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 197475 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 197475 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 197475 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 189145 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 189145 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 51059 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 51059 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 13801 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 13801 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 13801 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 120757 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 120757 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 27425 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 27425 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 28900 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 28900 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 194730 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 194730 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 26767 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 26767 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 108868 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 108868 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 16509 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 16509 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 2866 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 2866 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 2866 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 2866 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 2866 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 204577 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 204577 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 206582 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 206582 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 103164 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 103164 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 204538 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 204538 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 103164 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 103164 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 204538 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 204538 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 9688 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 9688 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 76075 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 76075 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 76075 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 76075 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 12464 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 12464 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 12464 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 46750 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 46750 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 19077 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 19077 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 172691 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 172691 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 172691 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 30911 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 30911 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 162741 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 162741 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 153740 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 153740 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 1581 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 1581 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 1581 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 1581 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 1581 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 119368 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 119368 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 119296 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 119296 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 173377 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 173377 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 15523 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 15523 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 118179 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 118179 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 12046 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 12046 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 12046 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 12368 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 12368 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 12368 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 99085 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 99085 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 99085 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 211231 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 13537 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 13537 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 13537 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 27191 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 27191 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 206922 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 206922 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 206922 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 161917 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 161917 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 161917 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 161917 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 132490 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 132490 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 95647 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 95647 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 119552 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 119552 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 204463 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 204463 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 204463 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 204463 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 2876 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 2876 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 2876 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 150633 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 150633 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 101656 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 101656 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 26770 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 26770 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 167834 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 167834 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 85242 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 85242 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 98514 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 98514 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 15158 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 15158 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 76071 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 76071 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 155075 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 155075 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 76069 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 76069 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 76069 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 76069 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 56267 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 56267 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 3780 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 3780 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 3780 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 3780 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 3780 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 30491 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 30491 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 95774 19 None 1 13 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 95774 19 None 1 13 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 145327 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 145327 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 70561 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 70561 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 24574 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 24574 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 94347 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 94347 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 116567 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 116567 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 2914 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 2914 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 2914 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 2914 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 18550 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 18550 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 32129 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 32129 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 26845 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 26845 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 51091 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 51091 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 98421 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 98421 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 204451 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 204451 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 51091 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 51091 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 3549 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 3549 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 3549 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 3549 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 204576 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 204576 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 204576 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 204576 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 138410 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 138410 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 29086 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 29086 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 10091 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 10091 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 146325 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 146325 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 160250 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 160250 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 204435 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 204435 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 99673 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 99673 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 87513 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 87513 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 164878 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 164878 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 28732 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 28732 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 116542 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 116542 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 174558 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 174558 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 47740 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 47740 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 13088 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 13088 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 13088 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 97390 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 97390 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 97390 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 193325 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 193325 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 175587 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 175587 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 47972 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 47972 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 162372 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 162372 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 206337 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 206337 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 31366 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 31366 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 3747 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 3747 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 3747 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 3747 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 3747 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 3747 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 119562 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 119562 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 2182 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 2182 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 2182 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 2182 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 2182 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 26731 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 26731 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 204638 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 204638 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 204638 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 204638 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 78520 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 78520 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 107524 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 107524 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 27490 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 27490 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 16894 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 16894 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 76073 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 76073 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 67456 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 67456 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 4779 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 4779 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 12692 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 12692 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 12692 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 189099 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 189099 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
176 398 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 398 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 398 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 398 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 398 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 205513 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 205513 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 205513 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 12793 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 12793 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 12793 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 104750 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 104750 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 104750 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 104750 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 2514 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 2514 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 2514 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 2514 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 2514 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 163295 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 163295 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 75695 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 75695 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 9828 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 9828 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 109672 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 109672 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 109672 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 109672 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 76072 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 76072 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 204125 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 204125 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 188931 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 188931 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 204125 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 204125 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 168322 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 168322 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 185377 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 185377 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 192968 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 192968 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 192968 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 193019 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 193019 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 193019 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 193031 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 193031 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 193031 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 43455 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 43455 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 4152 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 4152 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 4152 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 4152 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 4152 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 118671 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 118671 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 118671 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 118956 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 118956 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 85455 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 85455 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 118959 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 118959 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 91599 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 91599 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 91599 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 91599 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 118963 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 118963 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 118955 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 118955 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 118964 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 118964 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 2876 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 2876 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 2876 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 118958 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 118958 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 100107 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 100107 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 100107 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 162277 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 162277 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 162277 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 118963 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 118963 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 118952 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 118952 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 118954 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 118954 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 118964 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 118964 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 118961 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 118961 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 118957 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 118957 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 118953 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 118953 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 118275 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 118275 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 118960 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 118960 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 202564 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 202564 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 2857 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 2857 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 2857 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 2857 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 2857 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 291 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 291 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
479 291 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 291 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 291 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 291 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 142282 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 142282 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 144031 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 144031 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 168705 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 168705 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 142351 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 142351 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
5 139 72 None -23442 54 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 139 72 None -23442 54 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 139 72 None -23442 54 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 139 72 None -23442 54 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 169313 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 169313 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 138118 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 138118 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 138118 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 102398 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 102398 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 102398 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 200226 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 200226 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 180984 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 180984 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 200579 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 200579 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 200643 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 200643 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 26833 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 26833 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 3618 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 3618 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 3618 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 101865 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 101865 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 201493 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 201493 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 174257 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 174257 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 73152 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 73152 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 73152 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 73152 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 73152 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 73152 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 73152 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 73152 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 73152 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 73152 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 73152 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 73152 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 73152 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 73152 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 73152 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 102667 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 102667 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 202754 19 None 2 28 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 202754 19 None 2 28 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 202754 19 None 2 28 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 202754 19 None 2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 73152 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 73152 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 73152 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 200407 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 200407 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 140188 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 140188 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 180773 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 180773 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 206399 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 206399 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 200381 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 200381 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 200608 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 200608 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 201261 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 201261 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 93366 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 93366 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 102398 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 102398 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 102398 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 93366 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 93366 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 132440 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 132440 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 162277 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 162277 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 162277 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 200639 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 200639 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 200324 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 200324 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 200408 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 200408 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 201338 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 201338 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 201534 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 201534 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 98265 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 98265 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 148043 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 148043 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 200351 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 200351 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 200707 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 200707 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 200829 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 200829 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 23349 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 23349 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 200289 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 200289 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 201256 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 201256 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 201316 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 201316 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 25651 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 25651 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 170072 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 170072 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 75173 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 75173 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 151865 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 151865 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 75173 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 75173 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 168238 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 168238 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 168238 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 168238 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 200188 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 200188 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 1529 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 1529 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 1529 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 1529 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 183148 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 183148 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 200259 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 200259 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 200378 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 200378 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 13348 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 13348 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 13348 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 13202 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 13202 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 13202 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 81237 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 81237 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 91599 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 91599 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 91599 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 91599 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 2876 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 2876 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 2876 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 192986 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 192986 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 192986 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 201536 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 201536 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 44009 0 None -2 6 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 44009 0 None -2 6 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 179583 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 179583 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3619 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 3619 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 3619 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 1529 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 1529 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 1529 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 1529 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 3549 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 3549 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 3549 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 3549 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 1529 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 1529 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 1529 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 1529 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 13370 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 13370 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 13370 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 13741 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 13741 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 13741 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 3549 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 3549 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 3549 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 3549 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 146348 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 146348 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 202754 19 None -5 28 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 202754 19 None -5 28 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 202754 19 None -5 28 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 202754 19 None -5 28 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 26215 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 26215 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 201194 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 201194 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 181164 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 181164 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 200830 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 200830 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 102232 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 102232 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 179476 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 179476 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 205 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 205 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 205 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 205 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 205 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 205 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 165934 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 165934 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 165934 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 165934 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 201418 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 201418 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 118671 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 118671 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 118671 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 26215 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 26215 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 17134 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 17134 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 201378 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 201378 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 129421 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 129421 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 169313 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 169313 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 116559 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 116559 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 1529 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 1529 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 1529 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 1529 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 1529 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 1529 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 1529 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 1529 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 169313 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 169313 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 169313 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 169313 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 169313 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 169313 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 169313 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 169313 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 102280 4 None -8 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 102280 4 None -8 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 102280 4 None -8 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 102280 4 None -8 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 166237 1 None -4 3 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 166237 1 None -4 3 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 1529 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 1529 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 1529 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 1529 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 3619 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 3619 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 3619 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 102280 4 None -8 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 102280 4 None -8 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 2502 22 None -5 34 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 2502 22 None -5 34 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 2502 22 None -5 34 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 2502 22 None -5 34 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 16303 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 16303 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 2914 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 2914 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 2914 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 2914 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 165149 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 165149 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 189681 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 189681 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 80162 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 80162 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 168741 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 168741 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 132442 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 132442 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 70600 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 70600 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 129412 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 129412 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 129417 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 129417 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 129437 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 129437 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 73087 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 73087 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 132478 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 132478 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 2914 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 2914 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 2914 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 2914 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 204657 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 204657 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 115224 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 115224 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 17452 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 17452 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 95774 19 None 1 13 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 95774 19 None 1 13 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 13239 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 13239 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 13239 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 3256 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 3256 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 3256 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 3256 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 3256 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 139542 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 139542 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 156625 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 156625 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 54225 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 54225 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 127808 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 127808 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 12918 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 12918 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 12918 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 172282 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 172282 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 4884 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 4884 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 139294 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 139294 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 198806 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 198806 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 166492 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 166492 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 167276 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 167276 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 35994 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 35994 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 207712 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 207712 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 202872 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 202872 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 143247 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 143247 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
228 445 28 None -4 24 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
33 445 28 None -4 24 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 445 28 None -4 24 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 445 28 None -4 24 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 445 28 None -4 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 129432 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 129432 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 40039 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 40039 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 13175 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 13175 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 13175 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 202474 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 202474 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 202474 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 141833 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 141833 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 206432 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 206432 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 208344 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 208344 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 208344 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 112884 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 112884 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 72996 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 72996 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 3941 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 3941 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 3941 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 177912 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 177912 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 176545 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 176545 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 176545 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 106390 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 106390 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 106390 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 100874 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 100874 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 164905 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 164905 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 98534 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 98534 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 124654 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 124654 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 124654 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 76064 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 76064 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 92196 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 92196 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 172585 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 172585 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 92196 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 92196 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 196966 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 196966 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 176288 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 176288 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 176288 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 41707 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 41707 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 176586 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 176586 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 176586 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 207841 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 207841 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 94875 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 94875 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 176679 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 176679 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 176679 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 132445 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 132445 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 132470 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 132470 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 98431 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 98431 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 106390 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 106390 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 106390 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 206358 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 206358 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 141821 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 141821 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 113721 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 113721 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 61055 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 61055 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 1662 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 1662 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 1662 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 1662 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 1662 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 80007 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 80007 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 141503 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 141503 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 152974 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 152974 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 138869 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 138869 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 166425 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 166425 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 48485 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 48485 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 166425 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 166425 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 123248 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 123248 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 123249 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 123249 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 109800 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 109800 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 16773 0 None -1412 12 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 16773 0 None -1412 12 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 30775 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 30775 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 99078 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 99078 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 99316 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 99316 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 116951 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 116951 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 113721 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 113721 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 84080 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 84080 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 156005 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 156005 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 159221 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 159221 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 113412 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 113412 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 185190 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 185190 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 31125 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 31125 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 58093 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 58093 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 58735 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 58735 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 59010 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 59010 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 97318 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 97318 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 5303 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 5303 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 187253 0 None -257039 3 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 187253 0 None -257039 3 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 195164 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 195164 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 196456 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 196456 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 140059 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 140059 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 158946 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 158946 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 159559 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 159559 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 54439 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 54439 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 176309 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 176309 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 176309 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 92198 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 92198 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 79603 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 79603 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 201833 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 201833 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 177279 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 177279 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 919 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
621 919 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
83 919 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 919 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 919 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 176447 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 176447 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 176447 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 176448 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 176448 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 176448 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 67100 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 67100 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 129419 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 129419 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 129419 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 129419 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 168474 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 168474 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -616 19 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 203057 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 203057 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 198061 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 198061 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 70601 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 70601 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 106406 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 106406 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 106406 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 176365 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 176365 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 176365 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 177654 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 177654 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 101065 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 101065 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 184056 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 184056 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 106406 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 106406 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 106406 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 94848 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 94848 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 132418 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 132418 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 111661 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 111661 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 58601 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 58601 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 47993 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 47993 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 51264 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 51264 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 132474 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 132474 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 2914 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 2914 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 2914 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 2914 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 129447 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 129447 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 87508 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 87508 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 2914 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 2914 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 2914 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 2914 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 191499 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 191499 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 200285 37 None -12022 10 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 200285 37 None -12022 10 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 200285 37 None -12022 10 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 1420 21 None -218 23 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 3590 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 3590 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 3590 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 3590 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 3590 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 182481 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 182481 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 80042 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 80042 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 79821 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 79821 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 80171 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 80171 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 150515 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 150515 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 138734 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 138734 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 147014 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 147014 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 13157 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 13157 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 13157 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 100179 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 100179 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 100179 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 132454 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 132454 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 138718 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 138718 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 198269 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 198269 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 132483 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 132483 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 111351 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 111351 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 206582 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 206582 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 132426 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 132426 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 132477 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 132477 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 3513 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 3513 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 3513 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 94743 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 94743 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 113348 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 113348 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 123247 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 123247 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 79500 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 79500 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 95774 19 None -4 13 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 95774 19 None -4 13 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 202605 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 202605 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 30864 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 30864 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 33271 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 33271 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 119404 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 119404 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 121147 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 121147 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 204803 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 204803 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 68336 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 68336 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 158259 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 158259 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 69308 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 69308 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 113410 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 113410 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 119648 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 119648 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 205302 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 205302 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 205302 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 205302 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 120803 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 120803 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 205302 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 205302 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 205302 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 205302 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 9440 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 9440 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 195080 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 195080 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 157475 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 157475 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 156953 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 156953 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 97126 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 97126 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 97126 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 169115 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 169115 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 205302 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 205302 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 13054 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 13054 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 13054 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 130471 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 130471 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 130471 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 205302 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 205302 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 198060 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 198060 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 167296 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 167296 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 13412 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 13412 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 13412 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 99401 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 99401 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 132451 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 132451 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 103294 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 103294 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 129452 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 129452 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
491 192 9 None -77624 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 192 9 None -77624 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 192 9 None -77624 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 3182 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 3182 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 3182 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 3182 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 3182 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 138990 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 138990 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 14021 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 14021 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 14021 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 13476 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 13476 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 13476 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 129443 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 129443 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 11226 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 11226 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 11226 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 162755 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 162755 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 13540 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 13540 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 13540 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 63453 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 63453 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 96662 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 96662 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 96662 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 203196 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 203196 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 100812 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 100812 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 100203 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 100203 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 86972 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 86972 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 70158 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 70158 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 177764 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 177764 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 199929 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 199929 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 137984 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 137984 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 75295 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 75295 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 20333 57 None -12 16 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 20333 57 None -12 16 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 176646 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 176646 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 176646 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 165097 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 165097 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 165231 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 165231 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 115189 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 115189 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 108615 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 108615 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 108615 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 181606 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 181606 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 176514 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 176514 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 176514 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 214017 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 206290 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 206290 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 206290 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 206290 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 129449 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 129449 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 117105 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 117105 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 139535 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 139535 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 80287 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 80287 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 156415 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 156415 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 129418 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 129418 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 132455 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 132455 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 100405 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 100405 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 106032 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 106032 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 142884 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 142884 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 9713 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 9713 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 91599 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 91599 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 91599 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 91599 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 4143 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 4143 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 4143 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 4143 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 4143 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 171685 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 171685 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 79979 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 79979 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 155720 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 155720 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 70154 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 70154 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 113405 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 113405 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 3256 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 3256 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 3256 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 3256 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 3256 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 71904 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 71904 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 115120 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 115120 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 67785 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 67785 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 67785 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 84071 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 84071 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 192067 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 192067 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 66479 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 66479 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 66479 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 158415 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 158415 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 121867 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 121867 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 121870 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 121870 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 69195 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 69195 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 31219 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 31219 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 140159 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 140159 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 9660 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 9660 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 31219 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 31219 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 184341 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 184341 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 187286 0 None -20417 3 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 187286 0 None -20417 3 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 187512 0 None -5888 3 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 187512 0 None -5888 3 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 91059 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 91059 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 158539 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 158539 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 90983 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 90983 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 91234 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 91234 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 152468 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 152468 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 207641 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 207641 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 58602 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 58602 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 176337 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 176337 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 176337 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 176515 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 176515 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 176515 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 207613 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 207613 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 177379 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 177379 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 115190 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 115190 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 3779 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 3779 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 3779 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 3779 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 3779 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 70167 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 70167 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 197886 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 197886 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 9369 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 9369 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 9369 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 14018 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 14018 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 14018 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 98450 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 98450 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 112631 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 112631 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 104369 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 104369 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 104369 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 104369 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 110557 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 110557 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 110557 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 207919 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 207919 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 176293 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 176293 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 176293 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 87510 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 87510 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 70163 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 70163 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 102473 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 102473 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 102473 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 57071 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 57071 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 202143 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 202143 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 18502 0 None -281 5 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 18502 0 None -281 5 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 18502 0 None -281 5 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 101854 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 101854 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 67733 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 67733 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 203570 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 203570 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 200322 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 200322 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 149543 0 None -2238 12 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 149543 0 None -2238 12 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 199783 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 199783 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 86368 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 86368 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 3183 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 3183 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 3183 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 3183 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 3183 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 29085 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 29085 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 116531 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 116531 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 132461 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 132461 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 78477 1 None -15 5 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 78477 1 None -15 5 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 176465 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 176465 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 176465 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 170643 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 170643 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 193031 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 193031 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 193031 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 8805 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 8805 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 8805 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 78477 1 None -15 5 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 78477 1 None -15 5 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 177747 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 177747 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 170111 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 170111 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 67239 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 67239 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 11384 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 11384 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 161917 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 161917 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 80237 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 80237 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 139792 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 139792 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 177777 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 177777 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 15269 0 None -3 3 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 15269 0 None -3 3 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 114788 0 None -3 3 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 114788 0 None -3 3 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 102730 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 102730 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 99519 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 99519 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 107067 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 107067 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 129423 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 129423 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 102730 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 102730 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 114788 0 None -3 3 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 114788 0 None -3 3 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 15269 0 None -3 3 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 15269 0 None -3 3 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 97665 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 97665 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 99702 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 99702 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 197904 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 197904 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 175270 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 175270 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 66458 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 66458 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 66458 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 14450 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 14450 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 203386 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 203386 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 32227 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 32227 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 116746 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 116746 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 97831 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 97831 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 66093 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 66093 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 84072 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 84072 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 156474 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 156474 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 156814 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 156814 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 113411 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 113411 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 113413 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 113413 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 113417 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 113417 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 119487 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 119487 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 214332 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 214631 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 214951 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 215070 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 120475 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 120475 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 4831 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 4831 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 6256 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 6256 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 110527 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 110527 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 13262 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 13262 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 112040 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 112040 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 66435 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 66435 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 66435 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 1661 26 None -29 18 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 1661 26 None -29 18 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 1661 26 None -29 18 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 1661 26 None -29 18 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 1661 26 None -29 18 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 1661 26 None -29 18 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 116531 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 116531 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 171507 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 171507 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 203386 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 203386 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 189779 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 189779 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 99540 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 99540 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 99540 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 99540 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 99540 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 99540 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 78518 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 78518 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 95837 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 95837 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 176348 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 176348 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 176348 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 198744 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 198744 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 177141 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 177141 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 18507 0 None -131 3 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 18507 0 None -131 3 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 112991 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 112991 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 76070 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 76070 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 76070 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 76070 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 729 40 None -436 36 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
35 729 40 None -436 36 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
403 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 190137 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 190137 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 67798 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 67798 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 176471 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 176471 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 176471 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 128720 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 128720 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 176292 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 176292 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 176292 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 29616 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 29616 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 178957 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 178957 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 177212 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 177212 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 144072 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 144072 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 207121 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 207121 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 140143 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 140143 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 171438 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 171438 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 66132 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 66132 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 18520 0 None -3019 8 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 18520 0 None -3019 8 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 18520 0 None -3019 8 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 184056 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 184056 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 26123 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 26123 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 214017 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 214017 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 132431 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 132431 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 3616 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 3616 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 3616 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 166259 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 166259 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 155055 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 155055 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 138760 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 138760 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 132473 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 132473 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 14637 0 None -5 3 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 14637 0 None -5 3 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 129430 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 129430 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 171908 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 171908 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 138161 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 138161 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 66481 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 66481 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 66481 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 111779 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 111779 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 113426 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 113426 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 100409 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 100409 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 33487 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 33487 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 118786 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 118786 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 165369 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 165369 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 145213 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 145213 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 149295 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 149295 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 63850 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 63850 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 77747 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 77747 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 63850 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 63850 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 196687 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 196687 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 87731 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 87731 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 156196 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 156196 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 113418 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 113418 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 123244 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 123244 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 101713 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 101713 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 53623 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 53623 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 53935 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 53935 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 125189 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 125189 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 205013 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 205013 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 138574 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 138574 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 111340 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 111340 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 204943 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 204943 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 69009 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 69009 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 59146 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 59146 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 49930 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 49930 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 176627 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 176627 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 176627 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 2876 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 2876 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 2876 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 200912 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 200912 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 100310 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 100310 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 100310 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 194486 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 186118 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 186118 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 79948 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 79948 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 69576 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 69576 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 163424 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 163424 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 48294 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 48294 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 8659 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 8659 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 8659 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 206430 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 206430 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 206430 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 206430 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 43945 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 43945 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 177927 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 177927 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 203284 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 203284 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 176149 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 176149 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 176149 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 176149 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 132422 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 132422 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 80095 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 80095 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 163720 0 None -1819 6 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 163720 0 None -1819 6 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 100334 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 100334 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 79950 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 79950 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 79950 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 79950 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 165357 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 165357 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 81833 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 81833 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 78477 1 None -15 5 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 78477 1 None -15 5 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 114433 0 None -2 3 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 114433 0 None -2 3 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 2590 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 2590 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 2590 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 2590 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 2590 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 78477 1 None -15 5 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 78477 1 None -15 5 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 168100 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 168100 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 109010 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 109010 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 67799 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 67799 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 80086 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 80086 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 138694 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 138694 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 141461 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 141461 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 177795 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 177795 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 130682 1 None 1 5 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 130682 1 None 1 5 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 14637 0 None -5 3 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 14637 0 None -5 3 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 130682 1 None 1 5 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 130682 1 None 1 5 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 130682 1 None 1 5 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 130682 1 None 1 5 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 141215 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 141215 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 115196 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 115196 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 132459 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 132459 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 114433 0 None -2 3 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 114433 0 None -2 3 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 195930 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 195930 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 123245 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 123245 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 107560 0 None -4073 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 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 107560 0 None -4073 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 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 78160 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 78160 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 165930 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 165930 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 58598 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 58598 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 189518 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 189518 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 78160 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 78160 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 166606 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 166606 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 69310 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 69310 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 33487 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 33487 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 57240 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 57240 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 91943 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 91943 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 4795 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 4795 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 93130 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 93130 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 69318 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 69318 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 78423 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 78423 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 205720 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 205720 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 83593 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 83593 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 181191 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 181191 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 78195 0 None -4073 16 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 78195 0 None -4073 16 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 129304 0 None -24 3 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 129304 0 None -24 3 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 120931 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 120931 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 100264 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 100264 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 81833 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 81833 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 7469 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 7469 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 100722 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 100722 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 197962 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 197962 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 176645 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 176645 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 176645 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 161255 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 161255 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 198135 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 198135 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 125427 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 125427 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 16913 0 None -213 3 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 16913 0 None -213 3 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 13858 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 13858 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 13858 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 100971 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 100971 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 176541 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 176541 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 176541 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 79666 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 79666 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 66282 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 66282 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 102467 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 102467 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 102467 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 166853 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 166853 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 136451 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 136451 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 155718 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 155718 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 120052 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 120052 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 92199 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 92199 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 181917 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 181917 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 76074 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 76074 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 87506 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 87506 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 76074 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 76074 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 132480 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 132480 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 129453 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 129453 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 8937 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 8937 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 155503 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 155503 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 164933 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 164933 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 12241 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 12241 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 9752 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 9752 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 187103 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 187103 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 87731 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 87731 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 156120 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 156120 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 123242 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 123242 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 133575 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 133575 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
240 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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
660 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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 56259 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 56259 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 204805 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 204805 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 9660 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 9660 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 156753 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 156753 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 153053 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 153053 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 112030 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 112030 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 103295 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 103295 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 176394 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 176394 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 176394 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 176233 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 176233 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 176233 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 198094 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 198094 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 199715 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 199715 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 60524 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 60524 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 101922 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 101922 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 92195 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 92195 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 181426 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 181426 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 189800 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 189800 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 101643 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 101643 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 164965 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 164965 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 101643 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 101643 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 202054 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 202054 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 129463 0 None -15 3 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 129463 0 None -15 3 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 79894 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 79894 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 202960 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 202960 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 176311 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 176311 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 176311 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 181574 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 181574 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 79559 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 79559 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 101643 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 101643 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 101891 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 101891 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 100901 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 100901 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 181675 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 181675 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
180 401 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
200 401 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 401 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 401 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 401 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 194683 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 194683 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 3522 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 3522 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 3522 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 146770 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 146770 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 101891 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 101891 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 1662 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 1662 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 1662 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 1662 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 1662 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 100901 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 100901 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 194926 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 194926 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 104778 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 104778 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 189662 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 189662 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 920 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 920 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 920 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 920 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 100310 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 100310 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 100310 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 146578 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 146578 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 146578 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 146578 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 160640 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 160640 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 12888 0 None -5 3 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 12888 0 None -5 3 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 98584 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 98584 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 132437 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 132437 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 103193 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 103193 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 116559 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 116559 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 97628 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 97628 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 197838 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 197838 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 70172 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 70172 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 111786 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 111786 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 207628 0 None -3162 8 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 207628 0 None -3162 8 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 71076 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 71076 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 91949 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 91949 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 194683 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 194683 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 61173 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 61173 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 159230 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 159230 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 69307 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 69307 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 206594 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 206594 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 16257 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 16257 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 91058 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 91058 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 91052 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 91052 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 91799 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 91799 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 97897 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 97897 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 146382 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 146382 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 162236 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 162236 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 164965 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 164965 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 155561 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 155561 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 183809 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 183809 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 166528 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 166528 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 92195 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 92195 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 76063 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 76063 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 76063 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 76063 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 100086 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 100086 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 100086 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 200163 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 200163 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 7457 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 7457 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 102434 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 102434 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 25810 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 25810 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 132434 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 132434 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 82408 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 82408 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 102475 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 102475 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 102475 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 75296 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 75296 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 151869 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 151869 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 17453 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 17453 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 138730 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 138730 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 124327 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 124327 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 129048 0 None -17 8 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 129048 0 None -17 8 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 129048 0 None -17 8 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 129048 0 None -17 8 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 10486 0 None -3 3 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 10486 0 None -3 3 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 14637 0 None -5 3 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 14637 0 None -5 3 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 90983 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 90983 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 12607 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 12607 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 12607 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 31413 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 31413 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 101891 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 101891 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 61611 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 61611 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 78159 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 78159 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 168784 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 168784 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 58555 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 58555 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 161061 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 161061 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 206984 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 206984 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 109700 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 109700 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 113427 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 113427 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 69004 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 69004 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 58739 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 58739 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 139539 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 139539 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 176689 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 176689 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 176689 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 3548 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 3548 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 3548 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 203909 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 203909 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 100801 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 100801 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 186996 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 186996 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 3286 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 3286 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 3286 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 3286 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 3286 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 1657 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 1657 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 1657 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 1657 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 34687 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 34687 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 101920 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 101920 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 203207 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 203207 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 99420 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 99420 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 127539 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 127539 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
191 403 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
201 403 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 403 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 403 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 403 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 202045 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 202045 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 12956 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 12956 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 12956 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 185083 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 185083 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 61416 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 61416 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 108110 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 108110 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 87568 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 87568 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 176299 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 176299 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 176299 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 87507 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 87507 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 201301 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 201301 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 746 13 None -10 25 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
62 746 13 None -10 25 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 746 13 None -10 25 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 179865 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 179865 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 180859 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 180859 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 19995 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 19995 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 140842 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 140842 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 139899 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 139899 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 93401 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 93401 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 95229 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 95229 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 87571 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 87571 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 200574 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 200574 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 203324 9 None -3 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 203324 9 None -3 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 203324 9 None -3 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 203324 9 None -3 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 81581 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 81581 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 203324 9 None -3 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 203324 9 None -3 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 20884 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 20884 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 81581 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 81581 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 153144 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 153144 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 203174 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 203174 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 108869 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 108869 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 200466 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 200466 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 200911 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 200911 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 179839 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 179839 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 144389 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 144389 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 746 13 None -10 25 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
62 746 13 None -10 25 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 746 13 None -10 25 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 200503 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 200503 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 201348 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 201348 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 203174 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 203174 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 84412 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 84412 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 84412 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 100698 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 100698 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 100698 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 201309 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 201309 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 183324 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 183324 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 170810 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 170810 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 25685 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 25685 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 80174 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 80174 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 76073 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 76073 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 76073 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 76073 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 76073 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 76073 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 139109 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 139109 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 201339 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 201339 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 86109 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 86109 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 59966 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 59966 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 199480 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 199480 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 201305 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 201305 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 17134 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 17134 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 166575 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 166575 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 169313 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 169313 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 169313 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 169313 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 107366 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 107366 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 138424 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 138424 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 2914 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 2914 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 2914 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 2914 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 10486 0 None -3 3 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 10486 0 None -3 3 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 171469 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 171469 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 13652 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 13652 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 13652 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 13652 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 13652 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 13652 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 204638 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 204638 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 170010 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 170010 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 68396 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 68396 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 108587 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 108587 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 69298 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 69298 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 113423 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 113423 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 197765 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 197765 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 116633 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 116633 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 13856 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 13856 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 16773 0 None -1412 12 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 16773 0 None -1412 12 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 17170 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 17170 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 106064 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 106064 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 205819 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 205819 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 161691 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 161691 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 79955 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 79955 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 205819 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 205819 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 505 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
249 505 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 505 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 505 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 505 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 181767 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 181767 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 58550 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 58550 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 127167 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 127167 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 358 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
271 358 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
885 358 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 358 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 174421 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 174421 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 190066 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 190066 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 9585 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 9585 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 149527 0 None -14 11 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 149527 0 None -14 11 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 181635 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 181635 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 130471 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 130471 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 130471 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 17986 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 17986 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 17986 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 13480 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 13480 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 200127 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 200127 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 143264 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 143264 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 163432 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 163432 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 62353 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 62353 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 208 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 208 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 208 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3759 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 3759 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 3759 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 3759 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 95774 19 None -2 13 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 95774 19 None -2 13 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 166425 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 166425 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 98584 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 98584 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 78476 0 None -11 3 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 78476 0 None -11 3 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 3590 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 3590 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 3590 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 3590 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 3590 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 63841 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 63841 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 17553 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 17553 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 139646 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 139646 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 155873 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 155873 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 156114 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 156114 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 123243 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 123243 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 201995 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 201995 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 9752 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 9752 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 110646 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 110646 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 61601 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 61601 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 201995 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 201995 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 31035 0 None -3981 8 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 31035 0 None -3981 8 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 31035 0 None -3981 8 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 196451 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 196451 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 172633 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 172633 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 17690 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 17690 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 159080 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 159080 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 800 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 13414 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 13414 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 13414 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 205519 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 205519 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 97143 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 97143 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 78367 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 78367 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 93132 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 93132 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 7456 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 7456 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 155030 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 155030 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 199716 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 199716 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 114433 0 None -2 3 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 114433 0 None -2 3 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 119996 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 119996 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 102663 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 102663 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 3256 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 3256 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 3256 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 3256 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 3256 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 203053 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 203053 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 214014 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 214014 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 132462 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 132462 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 113957 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 113957 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 114433 0 None -2 3 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 114433 0 None -2 3 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 192968 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 192968 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 192968 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 120477 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 120477 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 14637 0 None -5 3 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 14637 0 None -5 3 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 80105 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 80105 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 80145 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 80145 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 82406 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 82406 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 16498 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 16498 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 70156 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 70156 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 78476 0 None -11 3 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 78476 0 None -11 3 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 100377 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 100377 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 127511 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 127511 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 140165 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 140165 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 63842 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 63842 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 61604 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 61604 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 63842 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 63842 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 63846 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 63846 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 113406 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 113406 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 113407 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 113407 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 57354 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 57354 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 31778 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 31778 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 77103 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 77103 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 66450 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 66450 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 66450 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 121874 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 121874 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 69295 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 69295 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 165288 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 165288 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 70779 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 70779 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 169110 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 169110 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 204743 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 204743 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 196335 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 196335 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 76562 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 76562 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 76564 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 76564 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 97495 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 97495 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 199015 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 199015 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 112034 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 112034 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 112034 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 112034 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 155480 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 155480 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 132425 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 132425 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 166685 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 166685 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 200832 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 200832 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 208600 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 132463 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 132463 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 206175 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 206175 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 17609 0 None -1148 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 17609 0 None -1148 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 116590 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 116590 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 155393 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 155393 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 80126 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 80126 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 86144 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 86144 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 100701 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 100701 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 143379 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 143379 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 143379 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 143379 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 76068 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 76068 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 132453 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 132453 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 28702 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 28702 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 202605 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 202605 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 62979 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 62979 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 35081 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 35081 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 139118 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 139118 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 61602 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 61602 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 63848 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 63848 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 159343 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 159343 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 61172 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 61172 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 121212 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 121212 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 69005 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 69005 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 59071 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 59071 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 120718 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 120718 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 186118 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 186118 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 176200 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 176200 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 176527 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 176527 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 176527 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 112032 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 112032 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 112032 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 112032 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 166953 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 166953 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 199811 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 199811 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 197888 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 197888 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 78067 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 78067 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 92199 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 92199 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 193806 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 139344 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 139344 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 70170 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 70170 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 10433 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 10433 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 44079 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 44079 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 203649 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 203649 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 38906 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 38906 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 181593 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 181593 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 59592 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 59592 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 94732 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 94732 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 19105 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 19105 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 138916 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 138916 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 166322 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 166322 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 132446 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 132446 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 129413 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 129413 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 98389 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 98389 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 58749 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 58749 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 155502 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 155502 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 158507 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 158507 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 111780 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 111780 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 203649 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 203649 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 63962 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 63962 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 17653 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 17653 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 69312 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 69312 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 102255 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 102255 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 96247 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 96247 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 108680 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 108680 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 169449 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 169449 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 166514 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 166514 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 87576 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 87576 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 119914 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 119914 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 193019 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 193019 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 193019 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 132427 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 132427 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 147160 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 147160 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 13858 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 13858 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 13858 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 171507 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 171507 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 206016 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 206016 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 190177 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 190177 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 143379 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 143379 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 2914 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 2914 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 2914 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 2914 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 109254 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 109254 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 14637 0 None -5 3 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 14637 0 None -5 3 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 154299 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 154299 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 75291 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 75291 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 81101 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 81101 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 2914 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 2914 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 2914 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 2914 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 63843 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 63843 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 195631 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 195631 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 158494 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 158494 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 123722 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 123722 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 69297 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 69297 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 124829 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 124829 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 78129 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 78129 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 181612 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 181612 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 63851 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 63851 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 160793 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 160793 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 54054 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 54054 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 98161 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 98161 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 91053 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 91053 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 107041 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 107041 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 181555 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 181555 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 53316 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 53316 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 53316 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 87573 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 87573 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 192297 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 192297 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 3655 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 3655 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 3655 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 167279 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 167279 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 92150 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 92150 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 16773 0 None -2454 12 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 16773 0 None -2454 12 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 139240 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 139240 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 185377 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 185377 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 70169 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 70169 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 205897 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 205897 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 80136 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 80136 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 177204 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 177204 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 91599 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 91599 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 91599 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 91599 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 115186 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 115186 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 115979 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 115979 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 13652 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 13652 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 132457 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 132457 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 203131 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 203131 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 13979 0 None -7 3 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 13979 0 None -7 3 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 14637 0 None -5 3 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 14637 0 None -5 3 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 9071 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 9071 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 112033 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 112033 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 111788 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 111788 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 113422 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 113422 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 207988 0 None -7585 9 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 207988 0 None -7585 9 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 87732 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 87732 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 79638 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 79638 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 121771 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 121771 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 121209 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 121209 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 93131 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 93131 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 173495 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 173495 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 107271 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 107271 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 66767 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 66767 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 13412 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 13412 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 13412 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 187918 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 187918 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 112033 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 112033 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 92202 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 92202 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 171507 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 171507 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 70171 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 70171 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 206424 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 206424 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 78767 0 None -36 3 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 78767 0 None -36 3 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 129440 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 129440 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 2866 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 2866 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 2866 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 2866 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 2866 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 181608 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 181608 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 14637 0 None -5 3 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 14637 0 None -5 3 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 70155 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 70155 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 13979 0 None -7 3 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 13979 0 None -7 3 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 14637 0 None -5 3 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 14637 0 None -5 3 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 77834 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 77834 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 195443 1 None -363 6 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 195443 1 None -363 6 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 195443 1 None -363 6 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 141411 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 141411 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 11906 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 11906 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 63847 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 63847 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 11906 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 11906 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 199063 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 199063 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 70543 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 70543 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 170643 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 170643 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 58554 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 58554 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 156233 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 156233 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 788 39 None -69 11 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 788 39 None -69 11 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 788 39 None -69 11 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 788 39 None -69 11 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 788 39 None -69 11 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 79839 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 79839 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 78100 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 78100 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 78100 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 78100 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 195235 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 195235 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 61416 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 61416 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 2532 43 None -91 58 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 132818 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 132818 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 112042 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 112042 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 206735 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 206735 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 113953 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 113953 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 13621 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 13621 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 13621 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 10178 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 10178 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 87567 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 87567 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 121027 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 121027 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 80163 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 80163 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 139244 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 139244 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 161917 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 161917 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 129450 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 129450 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 161917 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 161917 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 142885 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 142885 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 129427 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 129427 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 115979 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 115979 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 140165 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 140165 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 140165 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 140165 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 140165 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 140165 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 7523 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 7523 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 34697 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 34697 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 76075 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 76075 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 76075 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 76075 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 76075 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 76075 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 76075 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 76075 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 99740 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 99740 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 80685 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 80685 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 157468 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 157468 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 113408 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 113408 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 100163 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 100163 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 165712 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 165712 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 78177 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 78177 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 68334 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 68334 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 8578 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 8578 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 139564 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 139564 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 139909 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 139909 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 157589 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 157589 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 69296 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 69296 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 97951 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 97951 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 205302 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 205302 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 198674 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 198674 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 200103 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 200103 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 181259 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 181259 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 206397 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 206397 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 206397 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 206397 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 19077 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 19077 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 13339 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 13339 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 13339 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 3294 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 3294 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 3294 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 13540 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 13540 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 13540 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 201833 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 201833 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 129441 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 129441 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 132441 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 132441 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 48186 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 48186 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 4153 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 4153 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 4153 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 4153 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 4153 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 4906 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 4906 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 142885 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 142885 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 129429 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 129429 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 119277 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 119277 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 25810 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 25810 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 142129 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 142129 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 31035 0 None -3981 8 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 31035 0 None -3981 8 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 31035 0 None -3981 8 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 77310 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 77310 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 110646 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 110646 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 181608 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 181608 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 85574 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 85574 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 184342 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 184342 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 178235 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 178235 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 139902 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 139902 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 156618 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 156618 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 121213 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 121213 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 69309 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 69309 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 69319 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 69319 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 98001 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 98001 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 120332 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 120332 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 207942 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 207942 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 176446 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 176446 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 176446 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 152298 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 152298 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 12490 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 12490 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 113955 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 113955 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 174316 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 174316 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 66188 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 66188 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 81535 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 81535 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 12490 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 12490 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 176325 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 176325 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 176325 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 9294 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 9294 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 9294 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 1581 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 1581 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 1581 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 1581 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 1581 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 92202 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 92202 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 83807 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 83807 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 162214 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 162214 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 118275 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 118275 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 25651 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 25651 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 205 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 205 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 205 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 48469 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 48469 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 107029 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 107029 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 205 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 205 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 205 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 80137 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 80137 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 80137 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 80137 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 80239 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 80239 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 200733 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 200733 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 69816 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 69816 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 74699 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 74699 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 200538 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 200538 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 101865 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 101865 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 132473 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 132473 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 66127 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 66127 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 141323 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 141323 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 86109 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 86109 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 80159 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 80159 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 20647 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 20647 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 112119 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 112119 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 199444 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 199444 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 141780 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 141780 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 131800 1 None -13 3 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 131800 1 None -13 3 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 73395 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 73395 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 138630 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 138630 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 132423 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 132423 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 181003 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 181003 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 18951 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 18951 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 93367 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 93367 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 145327 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 145327 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 145327 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 145327 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 188974 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 188974 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 80247 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 80247 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 208 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 208 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 208 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 10239 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 10239 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 155756 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 155756 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 208 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 208 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 208 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 129415 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 129415 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 206063 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 206063 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 132448 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 132448 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 114461 0 None -7 5 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 114461 0 None -7 5 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 63844 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 63844 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 91052 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 91052 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 167166 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 167166 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 107312 0 None -776 8 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 107312 0 None -776 8 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 708 37 None -2041 19 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 708 37 None -2041 19 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 708 37 None -2041 19 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 91802 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 91802 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 110641 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 110641 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 33713 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 33713 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 138943 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 138943 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 48186 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 48186 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 103304 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 103304 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 155204 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 155204 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 93122 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 93122 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 155715 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 155715 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 166861 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 166861 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 200254 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 200254 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 177332 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 177332 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 199930 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 199930 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 119684 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 119684 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 106434 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 106434 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 106434 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 39653 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 39653 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 39653 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 203651 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 203651 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 203437 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 203437 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 100742 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 100742 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 176190 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 176190 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 146578 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 146578 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 146578 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 146578 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 211231 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 130471 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 130471 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 130471 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 9337 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 9337 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 9337 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 189835 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 189835 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 139794 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 139794 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 14031 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 14031 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 14031 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 149427 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 149427 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 114461 0 None -7 5 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 114461 0 None -7 5 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 132430 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 132430 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 106141 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 106141 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 205773 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 205773 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 106963 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 106963 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 87507 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 87507 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 91801 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 91801 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 141528 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 141528 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 138755 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 138755 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 206922 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 206922 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 206922 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 132413 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 132413 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 206079 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 206079 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 177314 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 177314 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 202474 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 202474 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 202474 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 205965 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 205965 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 79909 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 79909 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 151695 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 151695 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 132469 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 132469 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 13340 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 13340 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 13340 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 91599 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 91599 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 91599 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 91599 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 150633 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 150633 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 61610 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 61610 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 17691 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 17691 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 206807 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 206807 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 28549 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 28549 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 198080 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 198080 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 103410 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 103410 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 103410 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 103410 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 207617 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 207617 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 204963 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 204963 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 92204 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 92204 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 128155 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 128155 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 198134 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 198134 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 3370 62 None -74 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 3370 62 None -74 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 3370 62 None -74 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 3370 62 None -74 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 3370 62 None -74 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 206228 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 206228 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 187918 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 187918 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 92204 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 92204 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 95774 19 None -4 13 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 95774 19 None -4 13 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 95774 19 None -4 13 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 95774 19 None -4 13 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 116874 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 116874 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 132476 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 132476 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 196959 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 196959 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 125423 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 125423 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 109445 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 109445 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 4143 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 4143 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 4143 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 4143 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 4143 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 97252 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 97252 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 68332 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 68332 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 82161 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 82161 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 82161 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 133129 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 133129 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 66188 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 66188 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 58729 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 58729 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 8578 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 8578 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 9662 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 9662 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 121871 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 121871 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 120164 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 120164 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 91057 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 91057 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 98004 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 98004 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 113950 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 113950 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 87574 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 87574 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 159021 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 159021 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 132468 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 132468 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 76069 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 76069 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 76069 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 76069 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 92205 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 92205 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 800 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 800 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 800 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 800 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 800 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 800 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 132457 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 132457 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 25685 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 25685 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 129416 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 129416 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 108269 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 108269 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 108606 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 108606 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 2876 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 2876 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 2876 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 57943 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 57943 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 30139 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 30139 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 2876 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 2876 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 2876 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 181581 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 181581 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 181581 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 3940 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 3940 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 3940 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 2876 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 2876 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 2876 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 97727 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 97727 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 187711 0 None -4786 3 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 187711 0 None -4786 3 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 198118 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 198118 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 111342 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 111342 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 17874 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 17874 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 74694 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 74694 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 74694 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 2876 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 2876 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 2876 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 800 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 800 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 800 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 800 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 800 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 800 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 66959 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 66959 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 66959 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 56267 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 56267 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 92205 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 92205 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 132458 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 132458 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 12603 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 12603 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 12603 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 189554 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 189554 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 168611 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 168611 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 169056 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 169056 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 92203 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 92203 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 113539 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 113539 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 132471 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 132471 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 113959 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 113959 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 80309 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 80309 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 919 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
621 919 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
83 919 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 919 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 919 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 91599 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 91599 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 91599 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 91599 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 919 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
621 919 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
83 919 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 919 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 919 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 66125 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 66125 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 132482 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 132482 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 95774 19 None -4 13 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 95774 19 None -4 13 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 129438 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 129438 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 76071 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 76071 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 76071 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 76071 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 95341 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 95341 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 70548 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 70548 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 91996 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 91996 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 169056 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 169056 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 190227 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 190227 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 111790 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 111790 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 202873 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 202873 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 107047 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 107047 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 120349 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 120349 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 69010 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 69010 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 113951 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 113951 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 132467 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 132467 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 2914 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 2914 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 2914 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 2914 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 132419 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 132419 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 109449 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 109449 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 174061 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 174061 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 113421 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 113421 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 93129 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 93129 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 61171 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 61171 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 69300 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 69300 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 91055 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 91055 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 198674 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 198674 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 95907 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 95907 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 65246 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 65246 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 92201 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 92201 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 176445 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 176445 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 176445 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 12956 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 12956 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 12956 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 176587 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 176587 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 176587 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 192275 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 192275 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 56249 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 56249 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 202754 19 None -26 28 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 183203 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 183203 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 25810 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 25810 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 113954 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 113954 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 9768 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 9768 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 57938 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 57938 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 120351 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 120351 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 94820 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 94820 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 158853 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 158853 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 3281 61 None -10232 19 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 3281 61 None -10232 19 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 3281 61 None -10232 19 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 3281 61 None -10232 19 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 3281 61 None -10232 19 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 170028 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 170028 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 170028 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 177619 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 177619 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 206212 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 206212 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 99076 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 99076 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 167073 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 167073 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 146325 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 146325 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 128155 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 128155 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 92203 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 92203 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 168537 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 168537 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 115194 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 115194 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 81128 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 81128 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 200533 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 200533 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 167337 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 167337 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 132460 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 132460 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 132417 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 132417 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 93571 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 93571 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 32792 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 32792 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 180153 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 180153 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 61609 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 61609 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 194728 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 194728 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 66480 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 66480 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 66480 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 195706 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 195706 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 104752 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 104752 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 104752 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 104752 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 63852 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 63852 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 184245 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 184245 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 17489 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 17489 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 156105 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 156105 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 13259 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 13259 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 13259 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 93127 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 93127 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 132465 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 132465 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 69249 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 69249 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 194728 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 194728 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 194728 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 194728 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 189701 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 189701 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 114732 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 114732 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 133158 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 133158 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 160250 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 160250 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 47157 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 47157 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 112030 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 112030 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 120049 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 120049 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 106377 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 106377 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 106377 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 106422 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 106422 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 106422 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 141572 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 141572 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 12604 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 12604 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 12604 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 129428 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 129428 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 3256 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 3256 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 3256 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 3256 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 3256 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 96648 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 96648 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 63845 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 63845 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 67638 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 67638 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 67638 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 57160 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 57160 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 77266 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 77266 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 121210 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 121210 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 97896 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 97896 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 5473 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 5473 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 59054 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 59054 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 129445 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 129445 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 92201 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 92201 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 3613 27 None -5 18 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 113534 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 113534 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 103307 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 103307 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 169170 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 169170 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 102318 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 102318 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 106377 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 106377 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 106377 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 91978 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 91978 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 203023 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 203023 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 203023 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 203023 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 101061 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 101061 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 85883 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 85883 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 180833 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 180833 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 80036 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 80036 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 80078 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 80078 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 80258 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 80258 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 73087 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 73087 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 87575 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 87575 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 746 13 None -10 25 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
62 746 13 None -10 25 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 746 13 None -10 25 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 80036 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 80036 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 13955 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 13955 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 13955 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 129420 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 129420 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 132456 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 132456 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 87513 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 87513 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 149409 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 149409 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 7522 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 7522 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 87513 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 87513 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 746 13 None -10 25 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
62 746 13 None -10 25 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 746 13 None -10 25 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 100473 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 100473 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 200578 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 200578 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 73395 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 73395 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 73395 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 73395 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 87511 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 87511 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 73395 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 73395 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 129437 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 129437 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 129411 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 129411 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 206974 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 206974 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 201310 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 201310 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 129422 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 129422 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 12740 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 12740 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 12740 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 100698 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 100698 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 100698 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 63858 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 63858 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 63022 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 63022 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 137400 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 137400 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 102480 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 102480 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 102480 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 138807 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 138807 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 198269 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 198269 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 132474 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 132474 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 129451 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 129451 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 63854 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 63854 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 109184 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 109184 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 17652 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 17652 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 156591 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 156591 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 78425 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 78425 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 206141 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 206141 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 78111 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 78111 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 91978 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 91978 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 82408 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 82408 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 115192 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 115192 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 85880 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 85880 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 92197 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 92197 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 107083 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 107083 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 92197 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 92197 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 76563 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 76563 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 113541 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 113541 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 178158 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 178158 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 129450 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 129450 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 205573 3 None -134 12 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 205573 3 None -134 12 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 84074 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 84074 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 156962 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 156962 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 111446 0 None -5128 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 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 111446 0 None -5128 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 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
45482151 198009 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 198009 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 71926 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 71926 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 58329 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 58329 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 111191 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 111191 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 84076 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 84076 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 57831 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 57831 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 205573 3 None -134 12 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 205573 3 None -134 12 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 187215 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 187215 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 110219 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 110219 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 106404 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 106404 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 106404 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 2540 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 2540 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 2540 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 2540 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 2540 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 92200 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 92200 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 100967 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 100967 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 80150 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 80150 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 198387 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 198387 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 65078 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 65078 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -37 89 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
38 958 93 None -37 89 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
722 958 93 None -37 89 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 958 93 None -37 89 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 958 93 None -37 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 69313 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 69313 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 167797 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 167797 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 63961 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 63961 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 66472 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 66472 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 66472 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 76561 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 76561 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 12608 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 12608 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 12608 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 27282 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 27282 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 3256 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 3256 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 3256 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 3256 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 3256 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 3747 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 3747 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 3747 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 3747 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 3747 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 3747 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 182498 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 182498 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 9378 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 9378 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 9378 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 47919 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 47919 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 132447 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 132447 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 123665 0 None -41 3 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 123665 0 None -41 3 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 106422 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 106422 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 106422 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 198380 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 198380 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 132464 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 132464 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 139930 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 139930 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 140045 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 140045 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 159157 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 159157 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 98431 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 98431 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 94893 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 94893 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 111787 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 111787 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 93128 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 93128 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 92200 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 92200 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 188024 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 188024 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 98431 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 98431 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 98431 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 98431 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 2182 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 2182 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 2182 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 2182 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 2182 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 106404 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 106404 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 106404 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 102460 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 102460 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 102460 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 187890 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 187890 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 141413 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 141413 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 132481 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 132481 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 129431 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 129431 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 159755 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 159755 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 163173 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 163173 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 9088 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 9088 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 187547 0 None -190 3 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 187547 0 None -190 3 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 76573 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 76573 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 208137 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 208137 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 100801 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 100801 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 100801 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 100801 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 206426 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 206426 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 193118 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 193118 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 85903 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 85903 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 100801 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 100801 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 100801 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 100801 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 141688 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 141688 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 1465 72 None -154 39 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 97376 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 97376 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 98431 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 98431 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 13781 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 13781 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 13781 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 115198 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 115198 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 132415 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 132415 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 87281 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 87281 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 119344 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 119344 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 106122 0 None -7244 8 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 106122 0 None -7244 8 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 84075 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 84075 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 139793 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 139793 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 158582 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 158582 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 202874 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 202874 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 205720 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 205720 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 97366 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 97366 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 93126 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 93126 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 17931 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 17931 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 91054 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 91054 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 4779 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 4779 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 137987 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 137987 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 68012 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 68012 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 116569 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 116569 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 116569 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 63036 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 63036 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 13339 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 13339 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 13339 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
176 398 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 398 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 398 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 398 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 398 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 165038 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 165038 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 117490 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 117490 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 97524 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 97524 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 97524 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 97524 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 196148 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 196148 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 184840 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 184840 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 176982 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 176982 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 121211 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 121211 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 205513 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 205513 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 205513 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 110922 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 110922 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 56235 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 56235 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 106434 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 106434 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 106434 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 66290 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 66290 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 48520 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 48520 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 66290 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 66290 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 114382 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 114382 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 2914 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 2914 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 2914 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 2914 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 16257 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 16257 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 79897 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 79897 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 81314 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 81314 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 80077 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 80077 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 81314 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 81314 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 63373 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 63373 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 198038 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 198038 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 158139 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 158139 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 91997 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 91997 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 109184 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 109184 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 111191 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 111191 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 91061 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 91061 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 158634 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 158634 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 165932 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 165932 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 208026 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 208026 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 2514 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 2514 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 2514 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 2514 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 2514 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 196980 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 196980 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 163967 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 163967 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 202339 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 202339 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 139778 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 139778 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 48295 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 48295 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 163799 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 163799 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 102300 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 102300 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 141636 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 141636 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 12775 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 12775 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 12775 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 177826 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 177826 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 186976 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 186976 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 61607 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 61607 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 63856 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 63856 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 123720 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 123720 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 107047 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 107047 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 48295 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 48295 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 156105 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 156105 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 155712 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 155712 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 53785 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 53785 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 37505 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 37505 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 37505 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 17846 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 17846 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 138905 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 138905 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 28503 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 28503 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 110400 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 110400 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 203191 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 203191 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 132421 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 132421 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 181639 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 181639 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 176584 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 176584 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 176584 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 99519 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 99519 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 99519 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 99519 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 99880 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 99880 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 168842 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 168842 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 85242 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 85242 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 113424 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 113424 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 7554 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 7554 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 7554 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 7554 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 2876 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 2876 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 2876 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 78217 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 78217 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 31301 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 31301 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 10177 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 10177 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 187549 0 None -9549 3 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 187549 0 None -9549 3 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 17169 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 17169 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 69299 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 69299 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 76574 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 76574 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 199016 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 199016 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 141385 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 141385 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 70168 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 70168 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 203138 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 203138 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 56239 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 56239 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 145155 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 145155 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 109169 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 109169 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 109169 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 129422 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 129422 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 129436 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 129436 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 91599 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 91599 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 91599 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 91599 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 13340 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 13340 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 13340 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 118162 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 118162 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 76073 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 76073 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 69816 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 69816 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 109690 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 109690 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 151428 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 151428 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 4267 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 4267 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 106831 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 106831 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 132433 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 132433 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 22735 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 22735 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 181656 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 181656 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 87572 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 87572 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 3617 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 3617 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 3617 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 200033 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 200033 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 201057 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 201057 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 115233 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 115233 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 84413 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 84413 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 84413 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 200980 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 200980 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 62049 0 None -1 3 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 62049 0 None -1 3 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 172585 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 172585 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 919 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
621 919 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
83 919 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 919 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 919 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 153775 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 153775 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 3372 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 3372 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 3372 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 3372 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 3372 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 84081 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 84081 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 167172 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 167172 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 84077 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 84077 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 6985 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 6985 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 198119 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 198119 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 204402 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 204402 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 81116 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 81116 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 80050 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 80050 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 56241 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 56241 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 176363 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 176363 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 176363 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 74523 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 74523 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 181883 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 181883 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 132437 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 132437 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 171916 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 171916 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 139080 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 139080 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 80370 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 80370 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 113966 0 None -2 3 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 113966 0 None -2 3 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 100433 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 100433 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 100433 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 113966 0 None -2 3 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 113966 0 None -2 3 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 68333 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 68333 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 35083 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 35083 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 184451 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 184451 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 95053 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 95053 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 59013 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 59013 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 176199 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 176199 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 198882 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 198882 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 196980 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 196980 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 75013 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 75013 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 2914 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 2914 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 2914 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 2914 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 161887 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 161887 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 70161 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 70161 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 2914 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 2914 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 2914 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 2914 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 100265 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 100265 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 112805 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 112805 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 112805 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 129448 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 129448 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 76072 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 76072 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 69245 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 69245 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 13175 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 13175 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 13175 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 132412 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 132412 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 184562 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 184562 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 66326 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 66326 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 155312 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 155312 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 196135 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 196135 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 142015 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 142015 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 97519 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 97519 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 165321 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 165321 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 169464 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 169464 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 112035 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 112035 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 101643 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 101643 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 145219 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 145219 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 112035 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 112035 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 50949 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 50949 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 178755 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 178755 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 30736 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 30736 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 11641 0 None -1 3 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 11641 0 None -1 3 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 201833 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 201833 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 201833 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 201833 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 201833 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 201833 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 11641 0 None -1 3 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 11641 0 None -1 3 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 124438 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 124438 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 206313 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 206313 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 87509 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 87509 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 101007 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 101007 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 31755 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 31755 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 119293 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 119293 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 9440 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 9440 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 175277 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 175277 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 157852 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 157852 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 69443 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 69443 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 196980 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 196980 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 198882 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 198882 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 177442 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 177442 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 9275 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 9275 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 9275 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 2509 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 2509 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 2509 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 2509 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 2509 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 81212 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 81212 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 132480 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 132480 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 129434 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 129434 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 69302 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 69302 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 101004 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 101004 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 202564 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 202564 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 95317 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 95317 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 187511 0 None -7244 3 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 187511 0 None -7244 3 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 17585 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 17585 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 157803 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 157803 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 93124 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 93124 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 165156 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 165156 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 72745 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 72745 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 203275 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 203275 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 9262 92 None -89 21 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 9262 92 None -89 21 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 182182 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 182182 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 132479 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 132479 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 84592 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 84592 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 84592 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 118780 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 118780 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 113419 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 113419 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 1625 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 1625 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 1625 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 1625 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 1625 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 1625 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 91800 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 91800 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 78418 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 78418 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 176848 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 176848 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 91060 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 91060 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 1625 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 1625 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 1625 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 1625 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 1625 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 1625 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 198136 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 198136 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 28547 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 28547 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 954 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 954 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
701 954 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 954 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 954 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 91599 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 91599 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 91599 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 91599 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 80207 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 80207 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 81451 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 81451 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 12609 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 12609 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 12609 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 166893 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 166893 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 100109 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 100109 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 138375 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 138375 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 208008 0 None -2570 7 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 208008 0 None -2570 7 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 79693 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 79693 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 172282 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 172282 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 109210 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 109210 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 109210 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 164891 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 164891 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 166732 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 166732 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 174347 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 174347 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 182304 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 182304 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 198674 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 198674 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 87504 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 87504 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 198674 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 198674 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 169560 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 169560 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 202564 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 202564 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 166258 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 166258 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 9500 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 9500 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 9500 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 155666 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 155666 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 161151 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 161151 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 161151 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 138254 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 138254 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 205537 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 205537 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 124049 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 124049 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 124049 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 124049 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 67767 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 67767 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 152610 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 152610 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 177128 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 177128 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 132472 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 132472 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 132475 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 132475 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 186593 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 186593 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 13228 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 13228 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 13228 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 61605 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 61605 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 69301 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 69301 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 8130 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 8130 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 184956 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 184956 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 100928 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 100928 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 80187 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 80187 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 113960 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 113960 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 176433 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 176433 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 176433 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 151553 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 151553 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 91977 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 91977 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 200945 22 None -144 19 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 200945 22 None -144 19 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 200945 22 None -144 19 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 70160 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 70160 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 113420 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 113420 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 132481 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 132481 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 178046 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 178046 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 91560 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 91560 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 17523 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 17523 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 17552 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 17552 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 183899 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 183899 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 145216 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 145216 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 79726 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 79726 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 196161 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 196161 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 143562 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 143562 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 188949 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 188949 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 102858 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 102858 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 165045 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 165045 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 198083 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 198083 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 204345 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 204345 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 81059 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 81059 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 155056 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 155056 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 100107 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 100107 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 100107 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 70597 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 70597 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 95774 19 None -4 13 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 95774 19 None -4 13 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 87511 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 87511 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 3691 61 None -1 34 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 3691 61 None -1 34 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 3691 61 None -1 34 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 37686 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 37686 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 104861 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 104861 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 37686 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 37686 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 101363 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 101363 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 101363 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 102434 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 102434 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 87512 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 87512 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 84411 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 84411 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 84411 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 102434 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 102434 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 100801 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 100801 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 102434 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 102434 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 138742 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 138742 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 145896 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 145896 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 145896 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 145896 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 166532 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 166532 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 12606 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 12606 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 12606 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 132437 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 132437 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 79785 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 79785 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 137311 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 137311 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 86478 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 86478 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 78478 0 None -5 4 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 78478 0 None -5 4 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 78478 0 None -5 4 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 78478 0 None -5 4 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 9879 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 9879 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 65230 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 65230 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 156874 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 156874 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 69304 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 69304 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 68335 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 68335 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 110529 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 110529 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 156432 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 156432 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 35779 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 35779 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 118752 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 118752 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 93123 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 93123 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 203032 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 203032 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 11164 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 11164 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 164881 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 164881 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
490 191 8 None -30902 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 191 8 None -30902 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 191 8 None -30902 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 13652 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 13652 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 73386 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 73386 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 115187 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 115187 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 164033 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 164033 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 69315 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 69315 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 9662 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 9662 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 110641 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 110641 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 94849 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 94849 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 745 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
36 745 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
437 745 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 745 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 745 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 165249 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 165249 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 107425 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 107425 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 107425 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 205499 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 205499 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 203245 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 203245 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 203245 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 107425 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 107425 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 107425 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 91979 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 91979 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 80035 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 80035 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 79845 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 79845 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 115188 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 115188 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 202045 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 202045 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 123246 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 123246 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 97174 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 97174 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 78478 0 None -5 4 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 78478 0 None -5 4 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 112379 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 112379 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 132444 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 132444 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 176698 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 176698 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 78478 0 None -5 4 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 78478 0 None -5 4 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 91977 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 91977 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 70402 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 70402 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 72493 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 72493 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 155245 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 155245 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 176364 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 176364 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 176364 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 115193 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 115193 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 22501 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 22501 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 187215 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 187215 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 176381 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 176381 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 176381 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 79786 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 79786 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 99849 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 99849 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 99849 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 3613 27 None 1 18 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 3613 27 None 1 18 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 3613 27 None 1 18 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 80108 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 80108 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 91599 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 91599 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 91599 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 91599 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 91599 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 91599 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 91599 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 91599 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 3613 27 None 1 18 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 3613 27 None 1 18 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 3613 27 None 1 18 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 76065 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 76065 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 76066 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 76066 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 76064 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 76064 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 61603 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 61603 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 70598 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 70598 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 69306 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 69306 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 146578 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 146578 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 146578 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 146578 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 78412 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 78412 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 139282 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 139282 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 155662 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 155662 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 84070 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 84070 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 84078 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 84078 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 187548 0 None -8511 3 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 187548 0 None -8511 3 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 112029 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 112029 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 112029 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 112029 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 194683 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 194683 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 198864 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 198864 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 176432 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 176432 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 176432 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 99277 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 99277 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 78018 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 78018 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 138955 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 138955 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 148323 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 148323 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 132424 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 132424 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 201808 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 201808 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 199014 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 199014 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 186976 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 186976 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 4247 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 4247 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 115195 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 115195 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 78217 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 78217 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 94847 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 94847 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 196689 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 196689 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 78424 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 78424 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 106371 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 106371 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 106371 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 206707 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 206707 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 113952 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 113952 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 56250 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 56250 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 163080 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 163080 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 13622 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 13622 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 13622 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 129439 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 129439 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 165604 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 165604 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 111787 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 111787 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 79891 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 79891 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 78422 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 78422 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 202754 19 None -2 28 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 168248 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 168248 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 47373 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 47373 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 203024 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 203024 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 56234 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 56234 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 206917 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 206917 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 174257 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 174257 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 79884 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 79884 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 139238 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 139238 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 151645 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 151645 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 196117 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 196117 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 78277 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 78277 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 78217 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 78217 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 166779 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 166779 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 97518 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 97518 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 9569 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 9569 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 47373 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 47373 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 184319 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 184319 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 195875 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 195875 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 195991 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 195991 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 61170 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 61170 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 140070 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 140070 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 113415 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 113415 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 102090 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 102090 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 71902 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 71902 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 207995 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 207995 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 129446 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 129446 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 17586 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 17586 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 100386 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 100386 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 177493 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 177493 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 106371 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 106371 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 106371 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 129414 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 129414 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 98431 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 98431 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 98431 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 98431 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 98431 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 98431 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 103123 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 103123 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 200465 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 200465 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 103123 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 103123 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 80391 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 80391 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 138666 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 138666 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 3616 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 3616 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 3616 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 201306 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 201306 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 198711 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 198711 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 80259 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 80259 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 87506 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 87506 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 87505 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 87505 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 116578 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 116578 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 139555 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 139555 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 132438 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 132438 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 80240 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 80240 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 153786 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 153786 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 128488 0 None -2 3 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 128488 0 None -2 3 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 79893 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 79893 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 138762 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 138762 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 183019 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 183019 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 205453 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 205453 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 76067 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 76067 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 129425 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 129425 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 149704 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 149704 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 2914 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 2914 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 2914 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 2914 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 100229 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 100229 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 98431 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 98431 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 201982 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 201982 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 98919 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 98919 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 77095 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 77095 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 76569 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 76569 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 49140 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 49140 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 49324 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 49324 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 112018 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 112018 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 13347 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 13347 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 13347 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 164108 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 164108 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 9392 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 9392 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 9392 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 177299 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 177299 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 138451 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 138451 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 60804 0 None -26 5 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 60804 0 None -26 5 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 9397 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 9397 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 155880 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 155880 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 78450 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 78450 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 109700 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 109700 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 78025 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 78025 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 195553 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 195553 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 53846 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 53846 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 208081 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 208081 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 187744 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 187744 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 156265 3 None -1548 15 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 156265 3 None -1548 15 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 99183 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 99183 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 213975 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 115199 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 115199 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 61075 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 61075 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 177304 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 177304 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 113403 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 113403 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 12934 0 None -10 5 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 12934 0 None -10 5 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 129442 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 129442 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 12934 0 None -10 5 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 12934 0 None -10 5 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 100974 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 100974 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 13937 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 13937 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 68655 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 68655 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 101008 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 101008 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 205787 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 205787 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 205787 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 205787 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 101617 0 None -4677 6 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 101617 0 None -4677 6 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 155529 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 155529 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 3261 23 None -16595 29 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 3261 23 None -16595 29 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 3261 23 None -16595 29 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 202891 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 202891 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 2241 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 2241 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 2241 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 203245 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 203245 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 203245 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 178033 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 178033 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 203661 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 203661 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 198059 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 198059 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 91599 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 91599 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 91599 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 91599 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 158866 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 158866 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 146756 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 146756 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 2876 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 2876 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 2876 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 13177 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 13177 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 13177 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 169928 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 169928 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 97447 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 97447 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 58594 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 58594 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 76781 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 76781 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 76781 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 167989 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 167989 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 76066 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 76066 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 76066 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 76066 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 154378 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 154378 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 84079 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 84079 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 69314 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 69314 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 144468 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 144468 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 101617 0 None -4677 6 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 101617 0 None -4677 6 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 204659 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 204659 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 46819 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 46819 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 171507 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 171507 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 63074 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 63074 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 97180 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 97180 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 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
10665177 23143 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 23143 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 7018 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 7018 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 198010 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 198010 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 56259 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 56259 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 166060 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 166060 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 168008 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 168008 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 32318 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 32318 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 78321 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 78321 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 158050 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 158050 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 58507 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 58507 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 189942 0 None -426 4 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 189942 0 None -426 4 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 189942 0 None -426 4 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 177362 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 177362 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 113956 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 113956 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 44360 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 44360 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 48943 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 48943 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 177571 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 177571 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 167314 0 None -107 14 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 167314 0 None -107 14 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -616 19 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 708 37 None -512 19 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 708 37 None -512 19 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 708 37 None -512 19 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 97225 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 97225 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 78123 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 78123 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 189783 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 189783 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 164675 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 164675 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 130184 0 None -27 3 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 130184 0 None -27 3 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 168486 0 None -18620 6 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 168486 0 None -18620 6 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 132452 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 132452 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 949 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 949 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
671 949 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 949 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 949 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 73376 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 73376 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 91979 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 91979 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 2325 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 2325 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 2325 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 2325 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 2325 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 115197 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 115197 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 151980 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 151980 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 147923 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 147923 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 138958 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 138958 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 156236 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 156236 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 93125 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 93125 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 118092 0 None -11748 6 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 118092 0 None -11748 6 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 18057 0 None -27 3 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 18057 0 None -27 3 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 3173 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 3173 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 3173 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 3173 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 3173 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 188844 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 188844 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 100507 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 100507 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 180504 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 180504 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 77652 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 77652 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 17171 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 17171 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 10101 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 10101 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 1301 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 1301 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 1301 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 1301 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 1301 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 81107 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 81107 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 2914 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 2914 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 2914 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 2914 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 195264 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 195264 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 101363 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 101363 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 101363 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 112036 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 112036 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 176599 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 176599 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 176599 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 57070 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 57070 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 141958 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 141958 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 194683 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 194683 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 115120 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 115120 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 28269 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 28269 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 115120 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 115120 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 132429 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 132429 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 166897 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 166897 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 169933 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 169933 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 3759 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 3759 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 3759 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 3759 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 3759 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 3759 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 3759 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 3759 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 108249 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 108249 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 18812 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 18812 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 75252 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 75252 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 3614 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 3614 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 3614 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 166425 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 166425 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 140882 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 140882 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 494 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
22 494 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 494 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 68018 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 68018 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 68018 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 95742 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 95742 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 165604 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 165604 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 157392 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 157392 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 166945 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 166945 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 166968 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 166968 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 76570 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 76570 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 203298 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 203298 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 208006 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 208006 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 8823 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 8823 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 8823 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 80046 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 80046 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 69305 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 69305 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 100433 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 100433 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 100433 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 54465 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 54465 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 69311 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 69311 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 9909 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 9909 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 9909 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 9909 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 66075 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 66075 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 66075 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 66075 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 168525 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 168525 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 106403 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 106403 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 106403 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 198116 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 198116 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 176323 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 176323 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 176323 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 140848 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 140848 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 132439 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 132439 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 132477 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 132477 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 132414 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 132414 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 132432 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 132432 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 123673 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 123673 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 165604 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 165604 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 9088 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 9088 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 3940 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 3940 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 3940 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 132428 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 132428 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 80170 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 80170 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 143118 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 143118 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 168494 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 168494 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 178217 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 178217 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 110219 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 110219 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 94874 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 94874 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 204802 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 204802 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 110068 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 110068 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 165038 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 165038 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 176526 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 176526 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 176526 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 138802 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 138802 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 80107 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 80107 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 154306 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 154306 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 112031 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 112031 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 4153 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 4153 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 4153 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 4153 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 4153 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 140086 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 140086 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 167797 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 167797 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 195426 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 195426 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 196526 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 196526 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 2914 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 2914 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 2914 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 2914 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 81475 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 81475 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 194932 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 194932 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 72056 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 72056 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 2325 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 2325 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 2325 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 2325 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 2325 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 80116 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 80116 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 141457 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 141457 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 79922 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 79922 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 113425 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 113425 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 132450 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 132450 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 13239 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 13239 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 13239 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 115156 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 115156 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 91031 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 91031 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 84073 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 84073 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 140101 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 140101 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 155880 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 155880 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 156705 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 156705 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 156260 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 156260 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 156260 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 35380 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 35380 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 35380 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 35380 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 155244 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 155244 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 159557 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 159557 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 165003 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 165003 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 1582 14 None -9549 28 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 178115 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 178115 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 106403 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 106403 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 106403 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 132466 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 132466 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 101643 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 101643 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 102124 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 102124 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 132436 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 132436 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 167894 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 167894 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 82698 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 82698 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 82698 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 63853 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 63853 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 78209 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 78209 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 59087 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 59087 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 3261 23 None -16595 29 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 3261 23 None -16595 29 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 3261 23 None -16595 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 3261 23 None -977 29 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 181425 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 181425 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 176585 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 176585 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 176585 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 187 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
31 187 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
7 187 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 187 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 175580 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 175580 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 60400 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 60400 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 80013 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 80013 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 178232 0 None -11 4 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 178232 0 None -11 4 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 178232 0 None -11 4 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 129423 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 129423 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 9962 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 9962 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 206099 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 206099 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 132420 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 132420 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 119395 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 119395 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 200285 37 None -12022 10 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 200285 37 None -12022 10 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 200285 37 None -12022 10 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 200285 37 None -32359 10 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 200285 37 None -32359 10 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 200285 37 None -32359 10 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 200285 37 None -32359 10 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 200285 37 None -32359 10 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 200285 37 None -32359 10 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 156339 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 156339 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 99164 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 99164 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 200322 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 200322 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 138603 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 138603 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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
180 401 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
200 401 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 401 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 401 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 401 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 99494 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 99494 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 139664 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 139664 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 58728 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 58728 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 203251 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 203251 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 176289 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 176289 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 176289 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 176626 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 176626 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 176626 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 178572 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 178572 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 203419 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 203419 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 100936 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 100936 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 100936 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 100936 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 155149 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 155149 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 80030 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 80030 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 102434 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 102434 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 61384 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 61384 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 75422 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 75422 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 132446 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 132446 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 75416 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 75416 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 4143 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 4143 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 4143 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 4143 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 4143 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 202853 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 202853 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 132435 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 132435 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 142967 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 142967 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 129417 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 129417 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 129435 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 129435 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 65078 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 65078 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 158992 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 158992 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 17618 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 17618 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 106064 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 106064 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 202979 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 202979 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 186427 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 186427 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 71915 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 71915 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 149063 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 149063 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 58595 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 58595 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 69303 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 69303 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 120367 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 120367 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 113958 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 113958 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 204514 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 204514 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 41526 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 41526 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 100180 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 100180 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 100180 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 132416 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 132416 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 71787 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 71787 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 61608 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 61608 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 100180 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 100180 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 100180 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 159304 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 159304 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 113409 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 113409 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 203118 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 203118 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 84593 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 84593 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 84593 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 181559 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 181559 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 101542 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 101542 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 177273 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 177273 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 129424 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 129424 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 176290 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 176290 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 176290 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 111789 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 111789 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 113416 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 113416 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 48839 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 48839 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 56253 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 56253 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 14014 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 14014 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 14014 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 132443 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 132443 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 176647 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 176647 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 176647 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 13828 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 13828 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 214061 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 184317 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 184317 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 198115 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 198115 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 92198 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 92198 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 214061 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 919 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
621 919 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
83 919 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 919 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 919 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 140051 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 140051 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 198129 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 198129 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 194728 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 194728 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 176291 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 176291 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 176291 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 129426 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 129426 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 17907 0 None -3019 9 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 17907 0 None -3019 9 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 198607 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 198607 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 78032 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 78032 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 111781 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 111781 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 57569 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 57569 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 206141 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 206141 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 181570 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 181570 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 111591 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 111591 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 82406 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 82406 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 80167 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 80167 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 139623 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 139623 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 167315 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 167315 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 63855 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 63855 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 102472 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 102472 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 102472 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 17488 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 17488 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 36201 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 36201 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 176260 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 176260 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 176260 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 204061 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 204061 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 207207 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 207207 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 80115 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 80115 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 56254 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 56254 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 2244 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 2244 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 2244 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 2244 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 2244 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 2244 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 157380 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 157380 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 2244 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 2244 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 2244 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 176232 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 176232 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 176232 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 176688 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 176688 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 176688 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
240 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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
660 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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 944 43 None - 24 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 2006 111 None - 45 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 3780 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 3780 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 3780 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 3780 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 3780 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 3805 58 None -16 55 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 1660 35 None -11 17 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 291 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 291 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
479 291 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 291 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 291 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 291 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 2857 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 2857 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 2857 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 2857 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 2857 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 4152 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 4152 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 4152 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 4152 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 4152 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 3549 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 3549 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 3549 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 3549 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 2 28 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 202754 19 3H-SCH23390 -2 28 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 216384 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 216382 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 3613 27 3H-SCH23390 1 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 1 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 1 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1243 3618 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 3618 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 3618 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 215960 0 3H-SCH23390 High -6 27 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 215960 0 3H-SCH23390 High -6 27 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 746 13 3H-SCH23390 -2 25 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 746 13 3H-SCH23390 -8 25 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
62 746 13 3H-SCH23390 -2 25 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
62 746 13 3H-SCH23390 -8 25 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 746 13 3H-SCH23390 -2 25 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 746 13 3H-SCH23390 -8 25 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 3619 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 3619 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 3619 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -3 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 202754 19 3H-SCH23390 -2 28 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 3616 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 3616 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 3616 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 216386 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 1301 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 1301 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 1301 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 1301 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 1301 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 2914 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 2914 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 2914 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 2914 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 95774 19 3H-SCH23390 1 13 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 95774 19 3H-SCH23390 1 13 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 100179 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 100179 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 100179 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 2914 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 2914 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 2914 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 2914 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 3805 58 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
202 1508 77 UNDEFINED -9 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 77 UNDEFINED -9 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 77 UNDEFINED -9 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 77 UNDEFINED -9 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 77 UNDEFINED -9 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2 3261 23 3H-SCH23390 -208 29 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 3261 23 3H-SCH23390 -208 29 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 3261 23 3H-SCH23390 -208 29 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 3490 27 3H-SCH23390 -19952 14 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 3490 27 3H-SCH23390 -19952 14 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 3490 27 3H-SCH23390 -19952 14 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 8984 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 8984 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 98498 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 98498 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 115213 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 115213 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 176762 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 176762 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 190776 6 3H-SCH23390 -1698 11 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 190776 6 3H-SCH23390 -1698 11 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 203066 87 UNDEFINED -25 40 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 203066 87 UNDEFINED -25 40 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 203127 52 UNDEFINED -1 27 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 52 UNDEFINED -1 27 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 215992 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 216019 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 217332 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 81 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 81 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 81 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
5 139 72 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1192 147 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 147 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 147 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 187 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
31 187 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
7 187 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 187 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 297 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
932 297 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 297 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
179 400 115 3H-SCH23390 -4365 49 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
179 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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
963 400 115 3H-SCH23390 -4365 49 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
963 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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 400 115 3H-SCH23390 -4365 49 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 796 119 3H-SCH23390 -48 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
489 796 119 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 796 119 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 796 119 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 796 119 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 1401 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 1401 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 1401 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 1401 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 1401 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 1412 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 1412 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 1412 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 1412 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 1412 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 1462 97 3H-SCH23390 -12882 27 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 1462 97 3H-SCH23390 -12882 27 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 1462 97 3H-SCH23390 -12882 27 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 1462 97 3H-SCH23390 -12882 27 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 1462 97 3H-SCH23390 -12882 27 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 1465 72 3H-SCH23390 Low -23 39 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681 1465 72 3H-SCH23390 -97 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 Low -23 39 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -97 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 Low -23 39 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -97 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 Low -23 39 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -97 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 Low -23 39 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -97 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1209 1658 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 1658 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 1658 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 1658 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 1658 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 1709 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 1709 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 1709 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 1709 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 1709 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 1709 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 1709 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 1841 48 3H-SCH23390 -43651 26 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 1841 48 3H-SCH23390 -43651 26 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 1841 48 3H-SCH23390 -43651 26 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 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-SCH23390 -1949 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
12575 1988 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 1988 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 1988 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 2013 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 2013 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 2013 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 2013 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 2013 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 2013 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 2013 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 2013 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 2013 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 2013 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 2315 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 2315 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 2315 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 2315 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 2315 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 2315 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 2315 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 2418 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 2418 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 2418 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 2481 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 2481 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 2481 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 2481 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 2498 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 2498 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 2498 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 2498 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 2498 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 2498 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 2498 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 2498 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 2498 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 2498 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 2514 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 2514 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 2514 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 2514 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 2514 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 2518 84 3H-SCH23390 -676 22 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 2518 84 3H-SCH23390 -676 22 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 2518 84 3H-SCH23390 -676 22 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 2518 84 3H-SCH23390 -676 22 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 2518 84 3H-SCH23390 -676 22 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 2590 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 2590 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 2590 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 2590 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 2590 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 2590 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 2590 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 2590 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 2590 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 2590 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 2724 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 2724 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 2724 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 2724 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 2724 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 2724 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 2858 51 3H-SCH23390 -54 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 2858 51 3H-SCH23390 -24 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 2858 51 3H-SCH23390 -54 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 2858 51 3H-SCH23390 -24 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 2858 51 3H-SCH23390 -54 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 2858 51 3H-SCH23390 -24 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 2862 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 2862 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 2862 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 2955 0 3H-SCH23390 -562 7 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 2955 0 3H-SCH23390 -562 7 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 2955 0 3H-SCH23390 -562 7 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 3095 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 3095 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 3095 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 3095 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 3095 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3096 58 3H-dopamine -3801 36 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 3096 58 3H-SCH23390 -3801 36 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 3125 71 3H-SCH23390 -52480 30 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 3125 71 3H-SCH23390 -52480 30 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 3125 71 3H-SCH23390 -52480 30 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 3125 71 3H-SCH23390 -52480 30 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 3125 71 3H-SCH23390 -52480 30 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 3132 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 3132 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 3132 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 3132 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 3132 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 3159 96 3H-SCH23390 -7585 40 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 3159 96 UNDEFINED -7585 40 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 3159 96 3H-SCH23390 -7585 40 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 3159 96 UNDEFINED -7585 40 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 3159 96 3H-SCH23390 -7585 40 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 3159 96 UNDEFINED -7585 40 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 3159 96 3H-SCH23390 -7585 40 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 3159 96 UNDEFINED -7585 40 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 3159 96 3H-SCH23390 -7585 40 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 3159 96 UNDEFINED -7585 40 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 3183 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 3183 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 3183 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 3183 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 3183 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 3187 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 3187 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 3187 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 3187 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 3187 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 3187 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 3187 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 3187 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 3202 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 3202 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 3202 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 3202 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 3202 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 3261 23 3H-SCH23390 Low -2089 29 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 3261 23 3H-SCH23390 -977 29 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 3261 23 3H-SCH23390 Low -2089 29 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 3261 23 3H-SCH23390 -977 29 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 3261 23 3H-SCH23390 Low -2089 29 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 3261 23 3H-SCH23390 -977 29 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 3262 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 3262 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 3262 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3281 61 3H-SCH23390 -2754 19 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3370 62 3H-SCH23390 -74 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 3H-SCH23390 -74 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 3H-SCH23390 -74 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 3H-SCH23390 -74 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 3H-SCH23390 -74 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
183782 3398 20 3H-SCH23390 -1737 13 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 3398 20 3H-SCH23390 -1737 13 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 3398 20 3H-SCH23390 -1737 13 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 3464 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 3464 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 3464 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 3464 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 3491 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 3491 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 3491 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -70 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3703 110 3H-SCH23390 -549 21 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 3804 49 3H-dopamine -4168 26 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 3804 49 3H-dopamine -4168 26 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 3804 49 3H-dopamine -4168 26 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 4127 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 4127 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 4127 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 4127 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 4127 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 4323 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 4323 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 4323 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 11255 65 3H-SCH23390 -2344 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1179 11255 65 3H-SCH23390 -2344 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1255743 11255 65 3H-SCH23390 -2344 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
2662 11384 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 11384 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 14467 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 14467 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 15561 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 15561 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 27097 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 27097 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 27112 30 3H-SCH23390 -38 42 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 27112 30 3H-SCH23390 -38 42 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 46800 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 46800 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 46800 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 58548 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 58548 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 70300 19 3H-SCH23390 -776 33 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 70300 19 3H-SCH23390 -776 33 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 70300 19 3H-SCH23390 -776 33 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 79638 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 79638 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 79944 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 79944 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 79944 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 79944 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 84636 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 84636 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 84653 36 3H-SCH23390 -138 23 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 84653 36 UNDEFINED -138 23 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 84653 36 3H-SCH23390 -138 23 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 84653 36 UNDEFINED -138 23 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 91835 10 3H-8-OH-DPAT -66069 45 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 91835 10 3H-8-OH-DPAT -66069 45 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 94233 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 94233 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 94818 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL253529 94818 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448062 94848 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
CHEMBL253737 94848 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
44448066 94875 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
CHEMBL253948 94875 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
44448068 94876 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 94876 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 98126 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 98126 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 98126 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 98126 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 98880 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 98880 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 98880 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 99382 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 99382 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 99382 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 99967 83 3H-SCH23390 -288 29 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 99967 83 3H-SCH23390 -288 29 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 112521 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 112521 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 119525 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 119525 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 133521 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 133521 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 140707 7 UNDEFINED -89125 36 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 140707 7 UNDEFINED -89125 36 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 153188 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 153188 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 155204 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL402517 155204 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448065 155480 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 155480 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 155530 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 155530 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 167791 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 167791 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 176715 106 3H-dopamine -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176715 106 3H-dopamine -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
44581146 176828 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 176828 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 182770 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 182770 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 186920 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 186920 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 186920 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 187745 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 187745 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 188023 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 188023 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 188036 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 188036 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 188275 124 3H-SCH23390 -147 32 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 188275 124 3H-SCH23390 -147 32 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 188275 124 3H-SCH23390 -147 32 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 190374 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 190374 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 190528 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 190528 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 192533 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 192533 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 193615 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 193615 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 195017 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 195017 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 195017 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 195017 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 195017 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 195017 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 196535 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 196535 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 198806 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 198806 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 200551 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 200551 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 200551 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 202274 22 3H-SCH23390 -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 3H-SCH23390 -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 3H-SCH23390 -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3036864 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 202754 19 3H-SCH23390 -26 28 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 203025 92 3H-SCH23390 -275 33 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 203025 92 3H-SCH23390 -275 33 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 203066 87 3H-SCH23390 -25 40 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 203066 87 3H-SCH23390 -25 40 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 203483 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 203483 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 203483 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 203655 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 203655 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 204687 20 3H-SCH23390 -97 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 204687 20 3H-SCH23390 -97 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 204718 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 204718 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 204841 11 3H-SCH23390 -194 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 204841 11 3H-SCH23390 -194 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 205341 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 205341 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 205341 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 205501 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 205501 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 205501 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 205582 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 205582 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 205582 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 205758 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 205758 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 206203 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 206203 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 206367 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 206367 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 206367 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 206367 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 206367 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 206666 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 206666 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 207509 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 207509 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 208041 42 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
6852400 215937 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 215937 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 215937 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 215937 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 215937 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 215937 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 215940 0 3H-SCH23390 -1778 19 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 215943 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 215945 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 215945 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 215945 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 215945 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 215945 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 215945 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 215949 0 3H-SCH23390 -457 13 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 215949 0 3H-SCH23390 -457 13 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 215953 0 3H-SCH23390 -3467 58 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 215962 0 3H-dopamine -43651 16 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 215979 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 215990 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 215991 0 3H-SCH23390 -112201 14 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 215992 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 215993 0 3H-SCH23390 -1 28 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 215994 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 216019 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 216027 0 3H-SCH23390 -10 12 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 216037 0 3H-SCH23390 -70794 12 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 216129 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 216135 0 3H-SCH23390 -10471 24 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 216179 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 216179 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 216234 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 216239 0 3H-SCH23390 -95499 30 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 216254 0 3H-dopamine -8317 19 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 216286 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 216311 0 3H-SCH23390 -1 33 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 216312 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216315 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 0 3H-SCH23390 -1 39 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 216317 0 3H-SCH23390 -1 38 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 216318 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 216325 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 216326 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 216328 0 3H-SCH23390 -16 28 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 216329 0 3H-SCH23390 -3 28 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 216330 0 3H-SCH23390 -281 28 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 216331 0 3H-SCH23390 -1 28 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 216342 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 216389 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 216390 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 216391 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 216392 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 216393 0 3H-SCH23390 -1412 26 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 216394 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 216395 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 216450 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 216450 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 216489 0 3H-SCH23390 -4570 27 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 216494 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 216567 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 216720 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 216722 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 216723 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 216724 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 216732 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 216733 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 216772 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 217160 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 217272 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 217273 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 217515 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 217516 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 217517 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 217518 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 217519 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 217520 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 217521 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 217522 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 217523 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 217524 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 217525 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 217526 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 217527 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 217528 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 217529 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 217537 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 217538 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 215960 0 UNDEFINED -147 27 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 215960 0 UNDEFINED -147 27 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 215989 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 3613 27 3H-SCH23390 -6 18 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 -6 18 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 -6 18 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1353 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 196966 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 196966 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 215960 0 3H-SCH23390 Low -6 27 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 215960 0 3H-SCH23390 Low -6 27 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 297 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
932 297 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 297 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 1662 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 1662 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 1662 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 1662 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 1662 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 1465 72 3H-dopamine -23 39 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-dopamine -23 39 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-dopamine -23 39 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-dopamine -23 39 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-dopamine -23 39 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 216719 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 919 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
621 919 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
83 919 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 919 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 919 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 3616 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 3616 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 3616 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 919 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
621 919 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
83 919 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 919 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 919 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 216959 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 1301 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 1301 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 1301 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 1301 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 1301 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 1911 93 3H-SCH233930 -38 83 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 1911 93 3H-SCH233930 -38 83 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 1911 93 3H-SCH233930 -38 83 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 1911 93 3H-SCH233930 -38 83 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 1911 93 3H-SCH233930 -38 83 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 3590 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 3590 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 3590 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 3590 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 3590 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 1911 93 UNDEFINED -38 83 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 1911 93 UNDEFINED -38 83 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 1911 93 UNDEFINED -38 83 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 1911 93 UNDEFINED -38 83 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 1911 93 UNDEFINED -38 83 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 1301 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 1301 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 1301 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 1301 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 1301 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 3139 98 3H-dopamine -239 12 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 3139 98 3H-dopamine -239 12 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 3139 98 3H-dopamine -239 12 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 3139 98 3H-dopamine -239 12 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 3139 98 3H-dopamine -239 12 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 78179 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 78179 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 1465 72 UNDEFINED -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 UNDEFINED -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 UNDEFINED -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 UNDEFINED -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 UNDEFINED -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 217365 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 3256 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 3256 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 3256 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 3256 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 3256 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 181606 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 181606 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 3256 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 3256 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 3256 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 3256 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 3256 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 958 93 3H-SCH23390 -83 89 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
681 1465 72 125I-SCH 23982 -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 125I-SCH 23982 -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 125I-SCH 23982 -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 125I-SCH 23982 -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 125I-SCH 23982 -154 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 4143 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 4143 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 4143 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 4143 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 4143 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 216774 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 3256 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 3256 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 3256 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 3256 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 3256 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 4143 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 4143 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 4143 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 4143 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 4143 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 217363 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 3613 27 3H-SCH23390 Low -11 18 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 Low -11 18 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 Low -11 18 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
2105 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 2035 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 2035 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 2035 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 746 13 3H-SCH23390 -8 25 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
62 746 13 3H-SCH23390 -8 25 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 746 13 3H-SCH23390 -8 25 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 1664 49 3H-dopamine -2344 33 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 1664 49 3H-dopamine -2344 33 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 1664 49 3H-dopamine -2344 33 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 1664 49 3H-dopamine -2344 33 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 1664 49 3H-dopamine -2344 33 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 3653 50 3H-dopamine -31622 59 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 3653 50 3H-dopamine -31622 59 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 3653 50 3H-dopamine -31622 59 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 3653 50 3H-dopamine -31622 59 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 3653 50 3H-dopamine -31622 59 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 958 93 3H-SCH23390 -44 89 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -44 89 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -44 89 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -44 89 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -44 89 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
127708 112521 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 112521 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 2532 43 3H-SCH23390 -91 58 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-SCH23390 -91 58 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-SCH23390 -91 58 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-SCH23390 -91 58 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-SCH23390 -91 58 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
16362 3125 71 3H-SCH23390 -7413 30 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 3125 71 3H-SCH23390 -7413 30 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 3125 71 3H-SCH23390 -7413 30 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 3125 71 3H-SCH23390 -7413 30 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 3125 71 3H-SCH23390 -7413 30 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 1465 72 3H-SCH23390 -97 39 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -97 39 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -97 39 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -97 39 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -97 39 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
2389 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 216959 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 1911 93 UNDEFINED -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 UNDEFINED -74 83 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 216735 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 3613 27 3H-SCH23390 -5 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 -5 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 -5 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1890 2759 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 2759 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 2759 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 2759 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 2759 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 215979 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 215951 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 1911 93 3H-SCH23390 -107 83 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 1911 93 3H-SCH23390 -107 83 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 1911 93 3H-SCH23390 -107 83 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 1911 93 3H-SCH23390 -107 83 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 1911 93 3H-SCH23390 -107 83 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 2514 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 2514 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 2514 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 2514 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 2514 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 2348 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 2348 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 2348 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 2348 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 2348 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 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
33630 178957 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 178957 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 189518 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 189518 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 181191 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 181191 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 216773 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 3549 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 3549 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 3549 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 3549 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 216387 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 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-dopamine -23 39 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 216382 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 216726 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 117810 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 117810 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 3549 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 3549 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 3549 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 3549 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 202754 19 125I-Spectramide -2 28 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 202754 19 125I-Spectramide -2 28 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 202754 19 125I-Spectramide -2 28 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 202754 19 125I-Spectramide -2 28 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 3183 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 3183 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 3183 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 3183 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 3183 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 1662 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 1662 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 1662 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 1662 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 1662 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 920 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 920 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 920 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 920 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 1662 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 1662 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 1662 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 1662 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 1662 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 3613 27 3H-SCH23390 -1 18 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1242 3613 27 3H-SCH23390 1 18 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 -1 18 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 1 18 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 -1 18 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 1 18 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
135398737 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1662 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 1662 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 1662 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 1662 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 1662 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 2429 17 3H-SCH23390 -588 45 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 2429 17 3H-SCH23390 -588 45 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 2429 17 3H-SCH23390 -588 45 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 2429 17 3H-SCH23390 -588 45 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 2429 17 3H-SCH23390 -588 45 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 216282 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 216730 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 3805 58 3H-dopamine -309 55 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 2877 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2877 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2877 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
1153 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 216370 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 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1524 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 216284 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 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -44 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
242 470 124 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
242 470 124 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
34 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 470 124 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 470 124 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 470 124 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 2502 22 3H-SCH23390 -5 34 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 2502 22 3H-SCH23390 -5 34 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 2502 22 3H-SCH23390 -5 34 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 2502 22 3H-SCH23390 -5 34 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 216738 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 746 13 3H-SCH23390 -53 25 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
62 746 13 3H-SCH23390 -53 25 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 746 13 3H-SCH23390 -53 25 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 95774 19 3H-SCH23390 1 13 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 95774 19 3H-SCH23390 1 13 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 203174 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 203174 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 297 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
932 297 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 297 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 107531 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 107531 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 107531 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 107531 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 216177 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 95774 19 3H-SCH23390 -2 13 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 95774 19 3H-SCH23390 -2 13 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2181 96 3H-SCH23390 -338 52 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 2858 51 3H-dopamine 1 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 2858 51 3H-dopamine 1 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 2858 51 3H-dopamine 1 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 216721 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 181767 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 181767 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 174421 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 174421 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 190066 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 190066 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 1462 97 3H-SCH23390 -2630 27 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 1462 97 3H-SCH23390 -2630 27 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 1462 97 3H-SCH23390 -2630 27 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 1462 97 3H-SCH23390 -2630 27 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 1462 97 3H-SCH23390 -2630 27 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 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-dopamine -204 89 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
126968774 215989 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 67213 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 67213 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 1662 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 1662 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 1662 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 1662 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 1662 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 95774 19 3H-SCH23390 -4 13 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 95774 19 3H-SCH23390 -4 13 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 216385 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 2502 22 3H-dopamine -524 34 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 2502 22 3H-dopamine -524 34 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 2502 22 3H-dopamine -524 34 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 2502 22 3H-dopamine -524 34 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 3590 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 3590 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 3590 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 3590 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 3590 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 215960 0 UNDEFINED -147 27 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 215960 0 UNDEFINED -147 27 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 216736 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 216341 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2514 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 2514 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 2514 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 2514 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 2514 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 216233 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 954 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 954 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
701 954 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 954 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 954 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 3617 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 3617 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 3617 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 104780 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 104780 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 104780 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 104780 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 1662 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 1662 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 1662 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 1662 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 1662 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 176200 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 176200 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 1465 72 3H-SCH23390 -154 39 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -154 39 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -154 39 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -154 39 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -154 39 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1212 1662 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 1662 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 1662 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 1662 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 1662 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 107531 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 107531 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 107531 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 107531 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 216727 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 1662 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 1662 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 1662 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 1662 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 1662 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 3128 46 3H-SCH23390 -2041 35 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 3128 46 3H-SCH23390 -2041 35 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 3128 46 3H-SCH23390 -2041 35 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 3128 46 3H-SCH23390 -2041 35 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 3128 46 3H-SCH23390 -2041 35 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 217161 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 919 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 919 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
621 919 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
621 919 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
83 919 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
83 919 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 919 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 919 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 919 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 919 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 2914 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 920 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 920 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 920 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 920 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 2914 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 2914 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 2914 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 2914 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 2532 43 3H-dopamine -457 58 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-dopamine -457 58 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-dopamine -457 58 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-dopamine -457 58 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-dopamine -457 58 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 216960 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 216776 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 3613 27 3H-SCH23390 1 18 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 1 18 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 1 18 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
73333 5963 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 5963 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 2762 19 3H-SCH23390 -89125 19 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 2762 19 3H-SCH23390 -89125 19 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 2762 19 3H-SCH23390 -89125 19 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 3256 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 3256 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 3256 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 3256 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 3256 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 958 93 3H-SCH23390 -37 89 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -37 89 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -37 89 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -37 89 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -37 89 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 1911 93 3H-SCH23390 -30 83 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 1911 93 3H-SCH23390 -30 83 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 1911 93 3H-SCH23390 -30 83 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 1911 93 3H-SCH23390 -30 83 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 1911 93 3H-SCH23390 -30 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 216718 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 215938 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 217366 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 3780 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 3780 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 3780 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 3780 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 3780 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 291 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 291 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
479 291 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 291 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 291 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 291 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 958 93 3H-dopamine -204 89 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-dopamine -204 89 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-dopamine -204 89 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-dopamine -204 89 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-dopamine -204 89 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
125564 666 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
388 666 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 666 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 666 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 666 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 958 93 3H-SCH233930 -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH233930 -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH233930 -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH233930 -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH233930 -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 3057 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 3057 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 3057 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 3057 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 3057 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 958 93 UNDEFINED -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -44 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
134 2514 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 2514 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 2514 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 2514 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 2514 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 215960 0 UNDEFINED -144 27 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 215960 0 UNDEFINED -144 27 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 216729 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 216728 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 216957 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 4006 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 4006 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 4006 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 4006 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 205 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 205 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 205 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 746 13 3H-SCH23390 -10 25 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
62 746 13 3H-SCH23390 -10 25 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 746 13 3H-SCH23390 -10 25 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 199444 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 199444 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 1274 0 3H-SCH23390 -2 14 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 1274 0 3H-SCH23390 -2 14 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 1274 0 3H-SCH23390 -2 14 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 1274 0 3H-SCH23390 -2 14 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 1274 0 3H-SCH23390 -2 14 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 2429 17 3H-dopamine -97 45 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 2429 17 3H-dopamine -97 45 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 2429 17 3H-dopamine -97 45 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 2429 17 3H-dopamine -97 45 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 2429 17 3H-dopamine -97 45 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 4143 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 4143 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 4143 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 4143 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 4143 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 215953 0 3H-dopamine -426 58 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 3613 27 3H-SCH23390 High -11 18 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 High -11 18 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 High -11 18 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1427 2013 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 2013 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 2013 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 2013 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 2013 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 48186 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 48186 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 176190 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 176190 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 2914 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 2914 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 2914 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 2914 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 217364 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 1911 93 3H-SCH23390 -512 83 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 1911 93 3H-SCH23390 -512 83 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 1911 93 3H-SCH23390 -512 83 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 1911 93 3H-SCH23390 -512 83 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 1911 93 3H-SCH23390 -512 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 UNDEFINED -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 UNDEFINED -74 83 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 2532 43 3H-SCH23390 -457 58 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-SCH23390 -457 58 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-SCH23390 -457 58 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-SCH23390 -457 58 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-SCH23390 -457 58 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
6852400 215937 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 215937 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 1807 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 1807 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 1807 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 187918 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 187918 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 95774 19 125I-SCH 23982 -4 13 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 95774 19 125I-SCH 23982 -4 13 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 4143 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 4143 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 4143 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 4143 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 4143 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 3054 37 3H-SCH23390 -537 33 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 1662 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 1662 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 1662 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 1662 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 1662 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 216567 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 2877 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2877 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2877 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
135398745 2914 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 2914 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 2914 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 2914 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 95774 19 3H-SCH23390 -4 13 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 95774 19 3H-SCH23390 -4 13 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 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10707972 169056 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 169056 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 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 UNDEFINED -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -83 89 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2470 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 29616 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 29616 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 3653 50 3H-SCH23390 -10964 59 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 3653 50 3H-SCH23390 -10964 59 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 3653 50 3H-SCH23390 -10964 59 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 3653 50 3H-SCH23390 -10964 59 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 3653 50 3H-SCH23390 -10964 59 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 215965 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 94820 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 94820 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 215960 0 3H-SCH23390 -144 27 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 215960 0 3H-SCH23390 -144 27 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 3853 55 3H-SCH23390 -12 44 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 3853 55 3H-SCH23390 -12 44 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 3853 55 3H-SCH23390 -12 44 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 3853 55 3H-SCH23390 -12 44 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 3853 55 3H-SCH23390 -12 44 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 1465 72 3H-SCH23390 -97 39 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -97 39 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -97 39 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -97 39 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -97 39 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
13994416 190690 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 190690 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 3549 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 3549 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 3549 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 3549 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 205058 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 205058 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 3256 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 3256 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 3256 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 3256 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 3256 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 2181 96 3H-SCH23390 -301 52 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 2181 96 3H-SCH23390 -301 52 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 2181 96 3H-SCH23390 -301 52 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 2181 96 3H-SCH23390 -301 52 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 2181 96 3H-SCH23390 -301 52 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 2181 96 3H-SCH23390 -301 52 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 1660 35 3H-SCH23390 -2 17 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 746 13 3H-SCH23390 -10 25 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
62 746 13 3H-SCH23390 -10 25 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 746 13 3H-SCH23390 -10 25 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 3703 110 None -70 21 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 3370 62 None -74 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 None -74 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 None -74 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 None -74 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 None -74 24 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1212 1662 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 1662 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 1662 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 1662 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 1662 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 1662 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 1662 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 1662 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 1662 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 1662 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 3617 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 3617 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 3617 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 95774 19 3H-SCH23390 1 13 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 95774 19 3H-SCH23390 1 13 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 11384 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 11384 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 20333 57 None -12 16 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 20333 57 None -12 16 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 40039 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 40039 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 3054 37 3H-SCH23390 -645 33 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 215960 0 3H-SCH23390 -144 27 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 215960 0 3H-SCH23390 -144 27 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 82408 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 82408 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 958 93 3H-SCH23390 -169 89 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -169 89 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -169 89 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 958 93 3H-SCH23390 -169 89 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 958 93 3H-SCH23390 -169 89 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 3549 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 3549 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 3549 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 3549 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 55585 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 55585 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 3613 27 3H-SCH23390 1 18 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 1 18 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 1 18 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 596 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
312 596 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 596 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 596 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 596 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 2540 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 2540 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 2540 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 2540 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 2540 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 2006 111 3H-SCH23390 -56 45 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 3256 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 3256 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 3256 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 3256 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 3256 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 2532 43 3H-MIANSERIN -91 58 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-MIANSERIN -91 58 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-MIANSERIN -91 58 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-MIANSERIN -91 58 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-MIANSERIN -91 58 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 94893 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 94893 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 188024 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 188024 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 215960 0 3H-SCH23390 -147 27 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 215960 0 3H-SCH23390 -147 27 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 187890 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 187890 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 919 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
621 919 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
83 919 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 919 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 919 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 3057 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 3057 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 3057 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 3057 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 3057 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 216567 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 1465 72 3H-SCH23390 -154 39 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -154 39 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -154 39 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -154 39 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -154 39 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1222 1664 49 3H-SCH23390 -741 33 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 1664 49 3H-SCH23390 -741 33 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 1664 49 3H-SCH23390 -741 33 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 1664 49 3H-SCH23390 -741 33 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 1664 49 3H-SCH23390 -741 33 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 215971 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 3256 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 3256 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 3256 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 3256 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 3256 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 2914 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 2914 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 2914 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 2914 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 216775 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 216775 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 176982 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 176982 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 216232 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 2181 96 3H-SCH23390 -79 52 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 3373 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 3373 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 3373 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -4 17 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 1660 35 3H-SCH23390 -11 17 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 2877 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2877 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2877 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
6446379 216285 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 48295 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 48295 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 216739 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 3128 46 3H-dopamine -4073 35 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 3128 46 3H-dopamine -4073 35 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 3128 46 3H-dopamine -4073 35 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 3128 46 3H-dopamine -4073 35 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 3128 46 3H-dopamine -4073 35 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 216567 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 107531 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 107531 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 107531 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 107531 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 198864 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 198864 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 745 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
36 745 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
437 745 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 745 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 745 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 110529 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 110529 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
176 398 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 398 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 398 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 398 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 398 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 205513 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 205513 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 205513 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 4779 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 4779 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 3747 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 3747 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 3747 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 3747 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 3747 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 3747 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 2540 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 2540 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 2540 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 2540 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 2540 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 2540 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 2540 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 2540 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 2540 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 2540 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 160250 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 160250 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 206922 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 206922 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 206922 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 1581 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 1581 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 1581 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 1581 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 1581 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 3372 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 3372 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 3372 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 3372 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 3372 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 17986 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 17986 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 17986 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 800 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 800 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 800 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 800 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 800 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 800 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 505 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
249 505 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 505 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 505 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 505 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 1657 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 1657 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 1657 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 1657 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 3286 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 3286 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 3286 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 3286 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 3286 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
240 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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
660 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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 944 43 None -19 24 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 2590 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 2590 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 2590 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 2590 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 2590 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 216383 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 176149 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 176149 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 176149 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 176149 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 2532 43 None -46 58 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 3183 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 3183 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 3183 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 3183 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 3183 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 3779 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 3779 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 3779 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 3779 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 3779 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 3691 61 3H-SCH23390 -1 34 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 3691 61 3H-SCH23390 -1 34 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 3691 61 3H-SCH23390 -1 34 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 3182 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 3182 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 3182 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 3182 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 3182 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 1420 21 None -218 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 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 1420 21 None -218 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 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 1420 21 None -218 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 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 1420 21 None -218 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 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 1420 21 None -218 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 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 207841 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 207841 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 3331 118 UNDEFINED -346 67 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 206395 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 206395 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
5 139 72 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 216234 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 216234 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 215979 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 1465 72 3H-SCH23390 High -23 39 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 High -23 39 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 High -23 39 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 High -23 39 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 High -23 39 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
115237 55585 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 55585 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 297 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
932 297 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 297 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 2914 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 2914 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 2914 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 2914 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 216283 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 2914 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 2914 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 2914 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 2914 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 216737 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 217271 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 958 93 UNDEFINED -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5568 197500 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 197500 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 197500 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 197500 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 4006 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 4006 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 4006 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 4006 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 958 93 3H-SCH23390 -44 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -44 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -44 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -44 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -44 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2348 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 2348 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 2348 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 2348 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 2348 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 958 93 3H-SCH23390 -83 89 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954259 215979 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 216567 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 2006 111 3H-SCH23390 -794 45 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 2006 111 3H-SCH23390 -794 45 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 2006 111 3H-SCH23390 -794 45 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 2006 111 3H-SCH23390 -794 45 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 2006 111 3H-SCH23390 -794 45 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 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-SCH23390 -23 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
135398737 958 93 3H-SCH23390 -22 89 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-SCH23390 -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -22 89 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -22 89 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -22 89 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -22 89 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 176848 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 176848 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 3613 27 125I-SCH 23982 -5 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 125I-SCH 23982 -5 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 125I-SCH 23982 -5 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
24949693 182304 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 182304 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 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3331 118 3H-SCH233930 -489 67 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 3331 118 3H-SCH233930 -489 67 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 3331 118 3H-SCH233930 -489 67 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 3331 118 3H-SCH233930 -489 67 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 3331 118 3H-SCH233930 -489 67 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 3653 50 3H-SCH23390 -4168 59 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 2914 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 2914 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 2914 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 2914 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 3331 118 UNDEFINED -489 67 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 3331 118 UNDEFINED -489 67 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 3331 118 UNDEFINED -489 67 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 3331 118 UNDEFINED -489 67 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 3331 118 UNDEFINED -489 67 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 3805 58 3H-SCH23390 -16 55 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 216327 0 3H-SCH23390 16 28 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 2532 43 None -91 58 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -91 58 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -91 58 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -91 58 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -91 58 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 216734 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 215953 0 None -3467 58 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 949 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 949 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
671 949 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 949 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 949 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 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 803 103 None -112 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 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
31101 729 40 None -436 36 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
35 729 40 None -436 36 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
403 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 95774 19 3H-SCH23390 1 13 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 95774 19 3H-SCH23390 1 13 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 102858 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 102858 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 200945 22 None -144 19 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 200945 22 None -144 19 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 200945 22 None -144 19 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 9262 92 None -89 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 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9262 92 None -89 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 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
150 2509 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 2509 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 2509 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 2509 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 2509 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 3372 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 3372 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 3372 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 3372 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 3372 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 28724 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 28724 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 82408 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 82408 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 2514 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 2514 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 2514 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 2514 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 2514 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 2182 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 2182 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 2182 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 2182 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 2182 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 27282 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 27282 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 958 93 None -204 89 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
38 958 93 None -204 89 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
722 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -204 89 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 958 93 None -37 89 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
38 958 93 None -37 89 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
722 958 93 None -37 89 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 958 93 None -37 89 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 958 93 None -37 89 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 3256 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 3256 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 3256 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 3256 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 3256 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 66959 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 66959 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 66959 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 19077 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 19077 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 2866 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 2866 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 2866 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 2866 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 2866 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 217737 0 None 1 3 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 954 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 954 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
701 954 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 954 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 954 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 2006 111 None -56 45 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 3590 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 3590 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 3590 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 3590 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 3590 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 358 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
271 358 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
885 358 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 358 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
37 778 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
460 778 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 778 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 778 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 778 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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
191 403 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
201 403 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 403 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 403 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 403 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 2429 17 None -112 45 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 721 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 721 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 721 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 721 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 721 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 1465 72 None -97 39 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 178957 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 178957 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 14450 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 14450 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 958 93 None -44 89 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -44 89 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -44 89 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -44 89 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -44 89 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
277 1301 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 1301 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 1301 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 1301 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 1301 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 2492 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 2492 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 2492 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 2492 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 2492 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 3331 118 3H-SCH23390 -489 67 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 99323 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 99323 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 1581 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 1581 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 1581 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 1581 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 1581 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 216776 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 94849 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 94849 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 4006 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 4006 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 4006 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 4006 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 155245 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 155245 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 205527 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 205527 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 205527 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 3613 27 125I-SCH 23982 1 18 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 125I-SCH 23982 1 18 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 125I-SCH 23982 1 18 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1588 2325 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 2325 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 2325 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 2325 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 2325 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 155662 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 155662 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 216730 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 94847 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 94847 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 217367 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 216177 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 55585 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 55585 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 729 40 3H-SCH23390 -436 36 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
35 729 40 3H-SCH23390 -436 36 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
403 729 40 3H-SCH23390 -436 36 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 729 40 3H-SCH23390 -436 36 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 729 40 3H-SCH23390 -436 36 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 215960 0 3H-SCH23390 -144 27 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 215960 0 3H-SCH23390 -144 27 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 47373 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
CHEMBL154468 47373 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
134551 358 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
271 358 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
885 358 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 358 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 2914 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 2914 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 2914 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 2914 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 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 729 40 3H-SCH23390 -436 36 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
35 729 40 3H-SCH23390 -436 36 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
403 729 40 3H-SCH23390 -436 36 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 729 40 3H-SCH23390 -436 36 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 729 40 3H-SCH23390 -436 36 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 112521 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 112521 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
228 445 28 None -4 24 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
33 445 28 None -4 24 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 445 28 None -4 24 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 445 28 None -4 24 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 445 28 None -4 24 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 99323 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 99323 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 1662 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 1662 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 1662 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 1662 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 1662 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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 1911 93 None -30 83 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
180 401 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
200 401 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 401 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 401 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 401 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 2325 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 2325 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 2325 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 2325 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 2325 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 3173 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 3173 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 3173 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 3173 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 3173 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 919 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
621 919 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
83 919 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 919 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 919 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 215960 0 3H-dopamine -6 27 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 215960 0 3H-dopamine -6 27 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 2348 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 2348 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 2348 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 2348 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 2348 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
228 445 28 None -30 24 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
33 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 445 28 None -30 24 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 3806 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 3806 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 3806 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 3806 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 3806 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 958 93 None -83 89 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
38 958 93 None -83 89 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
722 958 93 None -83 89 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 958 93 None -83 89 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 958 93 None -83 89 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 112805 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 112805 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 112805 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 55585 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 55585 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 2914 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 2914 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 2914 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 2914 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 2496 52 None -30 42 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 919 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
621 919 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
83 919 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 919 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 919 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 4153 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 4153 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 4153 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 4153 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 4153 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 1662 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 1662 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 1662 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 1662 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 1662 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -346 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 3331 118 None -489 67 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 217711 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 1911 93 None -74 83 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 2914 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 2914 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 2914 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 2914 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 920 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 920 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 920 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 920 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 1660 35 None -34 17 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 67799 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 67799 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 102730 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 102730 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 3590 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 3590 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 3590 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 3590 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 3590 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 746 13 3H-dopamine -53 25 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
62 746 13 3H-dopamine -53 25 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 746 13 3H-dopamine -53 25 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 112521 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 112521 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 98020 77 3H-SCH23390 -371 34 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 98020 77 3H-SCH23390 -371 34 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 4153 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 4153 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 4153 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 4153 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 4153 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 3182 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 3182 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 3182 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 3182 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 3182 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 3256 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 3256 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 3256 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 3256 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 3256 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 187744 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 187744 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 215960 0 UNDEFINED -144 27 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 215960 0 UNDEFINED -144 27 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 155529 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 155529 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 1660 35 3H-SCH23390 -34 17 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 919 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
621 919 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
83 919 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 919 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 919 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 100179 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 100179 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 100179 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 2877 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2877 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2877 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2726 919 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
621 919 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
83 919 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 919 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 919 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 3860 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 3860 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 3860 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 3860 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 3860 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 3860 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 42802 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 42802 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3331 118 3H-SCH23390 -346 67 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 3805 58 3H-SCH23390 -309 55 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 3805 58 3H-SCH23390 -309 55 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 3805 58 3H-SCH23390 -309 55 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 3805 58 3H-SCH23390 -309 55 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 3805 58 3H-SCH23390 -309 55 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 217138 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 1911 93 3H-SCH23390 -52 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -52 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -52 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -52 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -52 83 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 1911 93 3H-SCH23390 -74 83 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 216415 0 3H-SCH23390 -691 6 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3125 71 3H-dopamine -30199 30 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 3653 50 3H-SCH23390 -31622 59 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 3653 50 3H-SCH23390 -31622 59 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 3653 50 3H-SCH23390 -31622 59 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 3653 50 3H-SCH23390 -31622 59 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 3653 50 3H-SCH23390 -31622 59 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 1465 72 3H-SCH23390 -1548 39 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-SCH23390 -1548 39 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-SCH23390 -1548 39 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-SCH23390 -1548 39 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-SCH23390 -1548 39 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 216958 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 3055 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 3055 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 3055 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 3055 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 3055 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 215960 0 3H-dopamine -6 27 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 215960 0 3H-dopamine -6 27 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 4143 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 4143 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 4143 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 4143 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 4143 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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 1465 72 None -23 39 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1274 0 None -2 14 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 1274 0 None -2 14 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 1274 0 None -2 14 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 1274 0 None -2 14 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 1274 0 None -2 14 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 215960 0 3H-dopamine -6 27 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 215960 0 3H-dopamine -6 27 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 203174 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 203174 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 107531 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 107531 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 107531 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 107531 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 746 13 3H-dopamine -53 25 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
62 746 13 3H-dopamine -53 25 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 746 13 3H-dopamine -53 25 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 199080 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 199080 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 216131 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 216725 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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 1660 35 3H-dopamine -34 17 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
180 401 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
200 401 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 401 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 401 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 401 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 2858 51 3H-dopamine 1 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 2858 51 3H-dopamine 1 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 2858 51 3H-dopamine 1 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 110529 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 110529 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 1911 93 3H-SCH23390 -38 83 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 94874 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 94874 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 1911 93 3H-SCH23390 -74 83 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 38278 0 3H-SCH23390 -2290 10 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 4153 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 4153 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 4153 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 4153 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 4153 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 3653 50 3H-SCH23390 -51286 59 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 958 93 3H-SCH23390 -83 89 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 1661 26 3H-SCH23390 -17 18 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 26 3H-SCH23390 -17 18 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 26 3H-SCH23390 -17 18 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
135398745 2914 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 2914 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 2914 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 2914 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 155244 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 155244 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 217133 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 215960 0 3H-SCH23390 -147 27 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 215960 0 3H-SCH23390 -147 27 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 958 93 3H-SCH23390 -83 89 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SCH23390 -83 89 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SCH23390 -83 89 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SCH23390 -83 89 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SCH23390 -83 89 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44591012 175580 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 175580 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 217137 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 9262 92 3H-dopamine -1318 21 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 9262 92 3H-dopamine -1318 21 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
180 401 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
200 401 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 401 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 401 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 401 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 958 93 UNDEFINED -44 89 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -44 89 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -44 89 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -44 89 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -44 89 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3805 58 3H-SCH23390 -47 55 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 3805 58 3H-SCH23390 -47 55 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 3805 58 3H-SCH23390 -47 55 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 3805 58 3H-SCH23390 -47 55 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 3805 58 3H-SCH23390 -47 55 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 1465 72 None -154 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 None -154 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 None -154 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 None -154 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 None -154 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 746 13 3H-SCH23390 -21 25 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
62 746 13 3H-SCH23390 -21 25 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 746 13 3H-SCH23390 -21 25 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 4143 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 4143 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 4143 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 4143 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 4143 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 95774 19 3H-SCH23390 1 13 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 95774 19 3H-SCH23390 1 13 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 919 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
621 919 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
83 919 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 919 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 919 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 215937 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 215937 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 216135 0 3H-KETANSERIN -9332 24 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1660 35 3H-SCH23390 -11 17 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 1911 93 3H-dopamine -512 83 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 216731 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 181559 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 181559 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 3332 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 3332 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 3332 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 3332 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 217368 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 919 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
621 919 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
83 919 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 919 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 919 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
5 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1242 3613 27 3H-SCH23390 -5 18 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-SCH23390 -5 18 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-SCH23390 -5 18 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
5281878 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1660 35 None -2 17 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 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
681 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
940 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
940 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
947 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
947 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
CHEMBL59 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
CHEMBL59 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
DB00988 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
DB00988 1465 72 None -154 39 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
5 139 72 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
5202 139 72 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
CHEMBL39 139 72 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
DB08839 139 72 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
1153 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
1242 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
935 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
935 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
CHEMBL286080 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL286080 3613 27 None -5 18 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
1712 2492 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 2492 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 2492 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 2492 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 2492 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 3173 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 3173 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 3173 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 3173 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 3173 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1628 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1911 93 None -38 83 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 1417 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 1417 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 1417 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 1417 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 3055 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 3055 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 3055 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 3055 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 3055 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 3759 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 3759 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 3759 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 3759 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 1529 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 1529 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 1529 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 1529 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3549 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 3616 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 3616 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 3616 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 208 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 208 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 208 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 3618 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 3618 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 3618 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 204405 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 None -23 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
5770 205058 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 205058 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3853 55 None -12 44 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 3780 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 3780 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 3780 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 3780 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 3780 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 2858 51 None -54 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 2858 51 None -54 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 2858 51 None -54 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 3372 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 3372 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 3372 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 3372 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 3372 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
228 445 28 None -35 24 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
228 445 28 None -35 24 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
33 445 28 None -35 24 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
33 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 445 28 None -35 24 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 297 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 297 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
932 297 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
932 297 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 297 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 297 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 3054 37 None -537 33 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 729 40 None -436 36 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 729 40 None -436 36 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
35 729 40 None -436 36 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
35 729 40 None -436 36 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
403 729 40 None -436 36 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
403 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 729 40 None -436 36 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 3615 0 None -1 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1826762
37 778 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
460 778 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 778 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 778 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 778 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 2181 96 None -79 52 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 3653 50 None -4168 59 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 3805 58 None -47 55 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 919 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
621 919 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
83 919 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 919 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 919 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 2325 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 2325 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 2325 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 2325 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 2325 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 2877 0 None -676 10 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 2877 0 None -676 10 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 2877 0 None -676 10 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 746 13 None -10 25 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 746 13 None -10 25 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
62 746 13 None -10 25 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
62 746 13 None -10 25 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 746 13 None -10 25 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 746 13 None -10 25 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 1662 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 1662 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 1662 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 1662 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 1662 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 3614 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 3614 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 3614 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