Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

216416 118358 48 None -117 23 Human 5.0 pAC50 = 5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 118358 48 None -117 23 Human 5.0 pAC50 = 5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
319 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 8106 44 None -3715 18 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
11504295 9697 47 None -75857 8 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
4814 9697 47 None -75857 8 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
7543 9697 47 None -75857 8 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
CHEMBL605846 9697 47 None -75857 8 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
DB09080 9697 47 None -75857 8 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
4151 10379 89 None -1819 10 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 10379 89 None -1819 10 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 10379 89 None -1819 10 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 10379 89 None -1819 10 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 10379 89 None -1819 10 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
2855 10904 104 None -5011 12 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
3322 10904 104 None -5011 12 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5717 10904 104 None -5011 12 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL603 10904 104 None -5011 12 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
DB00549 10904 104 None -5011 12 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
4066 211405 78 None -630 16 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 211405 78 None -630 16 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
242 7258 124 None -72 32 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -72 32 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -72 32 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -72 32 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -72 32 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
37 7565 60 None -89 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 7565 60 None -89 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 7565 60 None -89 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 7565 60 None -89 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 7565 60 None -89 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
6230 17092 63 None - 1 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 0 1 2 3.5 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1162 17092 63 None - 1 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 0 1 2 3.5 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
4746 211670 31 None -10 19 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 211670 31 None -10 19 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 211670 31 None -10 19 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
134 9292 24 None -1819 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 9292 24 None -1819 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 9292 24 None -1819 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 9292 24 None -1819 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 9292 24 None -1819 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
2335 18620 22 None -52 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None -52 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None -52 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None -52 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
60606 68334 73 None -5 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1771 68334 73 None -5 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
27812 73765 43 None 1 4 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 308 1 1 2 3.7 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21CC 10.1038/s41467-023-40064-9
CHEMBL1868702 73765 43 None 1 4 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 308 1 1 2 3.7 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21CC 10.1038/s41467-023-40064-9
2472 74058 48 None -19 4 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 1 7 2.1 CCCC(=O)N1CCCN(c2nc(N)c3cc(OC)c(OC)cc3n2)CC1 10.1038/s41467-023-40064-9
CHEMBL188185 74058 48 None -19 4 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 1 7 2.1 CCCC(=O)N1CCCN(c2nc(N)c3cc(OC)c(OC)cc3n2)CC1 10.1038/s41467-023-40064-9
5639 105671 75 None -218 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
CHEMBL279229 105671 75 None -218 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
447715 203706 68 None -18 7 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL566315 203706 68 None -18 7 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
1028 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 7079 71 None -10 19 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
2683 10606 60 None -1 6 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487 10606 60 None -1 6 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
7308 10606 60 None -1 6 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
CHEMBL1079 10606 60 None -1 6 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
DB00697 10606 60 None -1 6 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
68617 212306 62 None -10 30 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 212306 62 None -10 30 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 212306 62 None -10 30 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
10219 195575 37 None 1 10 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL493439 195575 37 None 1 10 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL50588 195575 37 None 1 10 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
102 10899 48 None 2 20 Human 7.9 pAC50 = 7.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None 2 20 Human 7.9 pAC50 = 7.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None 2 20 Human 7.9 pAC50 = 7.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None 2 20 Human 7.9 pAC50 = 7.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None 2 20 Human 7.9 pAC50 = 7.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
168871 95905 14 None -9 13 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 95905 14 None -9 13 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
17676 13844 29 None -275 13 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 13844 29 None -275 13 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 13844 29 None -275 13 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5472 212597 75 None -1 16 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 212597 75 None -1 16 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 212597 75 None -1 16 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
26248 168318 102 None -1 11 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
CHEMBL41286 168318 102 None -1 11 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
31703 201496 63 None -19 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL359744 201496 63 None -19 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL53463 201496 63 None -19 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2402 10143 62 None -616 16 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 10143 62 None -616 16 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 10143 62 None -616 16 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 10143 62 None -616 16 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 10143 62 None -616 16 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
441074 26186 82 None -9 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL1294 26186 82 None -9 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
1353 8692 93 None -2884 39 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -2884 39 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -2884 39 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -2884 39 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -2884 39 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3149 19386 15 None -35 26 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 19386 15 None -35 26 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
3316 38534 71 None -23 4 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
CHEMBL1405973 38534 71 None -23 4 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
636403 195047 22 None -5 7 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL499915 195047 22 None -5 7 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
179 7188 115 None -1905 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
2159 7188 115 None -1905 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
963 7188 115 None -1905 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
CHEMBL243712 7188 115 None -1905 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
DB06288 7188 115 None -1905 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
68712 107114 60 None 1 7 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
CHEMBL289480 107114 60 None 1 7 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
2105 9828 37 None -91 24 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None -91 24 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None -91 24 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None -91 24 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None -91 24 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
11079 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 9510 63 None -5 7 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3157 8252 71 None -5370 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 8252 71 None -5370 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 8252 71 None -5370 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 8252 71 None -5370 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 8252 71 None -5370 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
1212 8443 50 None -891 35 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 8443 50 None -891 35 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 8443 50 None -891 35 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 8443 50 None -891 35 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 8443 50 None -891 35 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
119570 9933 96 None -3019 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2233 9933 96 None -3019 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
953 9933 96 None -3019 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
CHEMBL301265 9933 96 None -3019 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
DB00413 9933 96 None -3019 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
4209 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 9937 75 None -19952 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
2780 117306 36 None -1479 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL325109 117306 36 None -1479 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
5453 210398 102 None -323 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 210398 102 None -323 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
4477 43310 90 None -13 4 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 3 2 4 3.9 O=C(Nc1ccc([N+](=O)[O-])cc1Cl)c1cc(Cl)ccc1O 10.1038/s41467-023-40064-9
CHEMBL1448 43310 90 None -13 4 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 3 2 4 3.9 O=C(Nc1ccc([N+](=O)[O-])cc1Cl)c1cc(Cl)ccc1O 10.1038/s41467-023-40064-9
214 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None -467 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
11626560 207716 94 None -16 14 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 207716 94 None -16 14 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
135398737 7745 93 None -112 43 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -112 43 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -112 43 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -112 43 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -112 43 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
1593 9119 66 None 1 6 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668 9119 66 None 1 6 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
9868 9119 66 None 1 6 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
CHEMBL17860 9119 66 None 1 6 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
DB04948 9119 66 None 1 6 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
1816 9318 102 None -39 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 9318 102 None -39 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 9318 102 None -39 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 9318 102 None -39 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 9318 102 None -39 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
2146 9874 67 None -123 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None -123 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None -123 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None -123 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None -123 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
13314 91008 15 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 1 1 3 3.1 CN1C(=O)C(O)N=C(c2ccccc2Cl)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
CHEMBL22097 91008 15 None -1 3 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 1 1 3 3.1 CN1C(=O)C(O)N=C(c2ccccc2Cl)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
2142 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 9870 58 None -11 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
2343 21226 57 None -1 4 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 431 5 2 6 2.2 NS(=O)(=O)c1cc2c(cc1Cl)N=C(CSCc1ccccc1)NS2(=O)=O 10.1038/s41467-023-40064-9
CHEMBL1201039 21226 57 None -1 4 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 431 5 2 6 2.2 NS(=O)(=O)c1cc2c(cc1Cl)N=C(CSCc1ccccc1)NS2(=O)=O 10.1038/s41467-023-40064-9
150 9287 21 None -2041 17 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 9287 21 None -2041 17 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 9287 21 None -2041 17 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 9287 21 None -2041 17 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 9287 21 None -2041 17 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
392622 63086 95 None -14 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 63086 95 None -14 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
68602 211905 80 None -10 4 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
CHEMBL77921 211905 80 None -10 4 Human 5.8 pAC50 = 5.8 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
1201549 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 7384 24 None -1584 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
6018 17837 96 None -2 3 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
CHEMBL117785 17837 96 None -2 3 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
2601 10552 33 None -5 17 Human 7.8 pAC50 = 7.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 10552 33 None -5 17 Human 7.8 pAC50 = 7.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 10552 33 None -5 17 Human 7.8 pAC50 = 7.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 10552 33 None -5 17 Human 7.8 pAC50 = 7.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 10552 33 None -5 17 Human 7.8 pAC50 = 7.8 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
4567 16720 34 None -239 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 16720 34 None -239 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
41684 37995 105 None -42 32 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 37995 105 None -42 32 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
25102847 84996 93 None -15 10 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 84996 93 None -15 10 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
443955 211149 92 None -17 8 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 350 3 0 4 4.1 CCOC(=O)C1=C[C@]2(CC)CCCN3CCc4c(n1c1ccccc41)[C@@H]32 10.1038/s41467-023-40064-9
CHEMBL71752 211149 92 None -17 8 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 350 3 0 4 4.1 CCOC(=O)C1=C[C@]2(CC)CCCN3CCc4c(n1c1ccccc41)[C@@H]32 10.1038/s41467-023-40064-9
16363 7383 53 None -3630 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 7383 53 None -3630 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 7383 53 None -3630 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 7383 53 None -3630 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 7383 53 None -3630 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2435 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
395 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
520 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
5386 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL844 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
DB00484 7509 100 None 7 10 Human 8.6 pAC50 = 8.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
82153 50675 45 None -41 3 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
CHEMBL1512 50675 45 None -41 3 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
11980903 21264 19 None -549 25 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 21264 19 None -549 25 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 21264 19 None -549 25 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 21264 19 None -549 25 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
610479 22272 90 None -2 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL121626 22272 90 None -2 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
2448 106099 70 None -912 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 106099 70 None -912 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
1830 9368 44 None -123 11 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 9368 44 None -123 11 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 9368 44 None -123 11 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 9368 44 None -123 11 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 9368 44 None -123 11 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
3081361 100709 123 None -3 14 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 100709 123 None -3 14 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
2318 161635 29 None -32 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 161635 29 None -32 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
154257 185398 67 None -10 19 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 185398 67 None -10 19 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
10102 9324 88 None -2089 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
1824 9324 88 None -2089 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
65906 9324 88 None -2089 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
CHEMBL94454 9324 88 None -2089 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
DB12523 9324 88 None -2089 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
4260 59332 31 None -20 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
CHEMBL159226 59332 31 None -20 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
53276 101809 53 None -1 5 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 304 5 3 5 3.0 CCOC(=O)Nc1ccc(NCc2ccc(F)cc2)nc1N 10.1038/s41467-023-40064-9
CHEMBL255044 101809 53 None -1 5 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 304 5 3 5 3.0 CCOC(=O)Nc1ccc(NCc2ccc(F)cc2)nc1N 10.1038/s41467-023-40064-9
5329102 201505 86 None -138 37 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None -138 37 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
4452 9538 19 None -8317 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 9538 19 None -8317 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 9538 19 None -8317 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
6337614 19768 54 None -22 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1189679 19768 54 None -22 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
1234 196000 56 None -95 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1256940 196000 56 None -95 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL51149 196000 56 None -95 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
65859 25821 88 None -2 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 236 4 2 4 0.2 OC[C@@H](O)CN1CCN(c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1288810 25821 88 None -2 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 236 4 2 4 0.2 OC[C@@H](O)CN1CCN(c2ccccc2)CC1 10.1038/s41467-023-40064-9
47979 84985 59 None -8709 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL2105581 84985 59 None -8709 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
68712 107114 60 None 1 7 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
CHEMBL289480 107114 60 None 1 7 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
1960 9632 67 None -13 19 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 9632 67 None -13 19 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 9632 67 None -13 19 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 9632 67 None -13 19 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 9632 67 None -13 19 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
4031 106089 28 None -4 12 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
CHEMBL282121 106089 28 None -4 12 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
31508 103993 38 None -2 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 278 2 0 3 4.0 Cc1ccc2c(-c3ccccc3)nc(=O)n(C(C)C)c2c1 10.1038/s41467-023-40064-9
CHEMBL268501 103993 38 None -2 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 278 2 0 3 4.0 Cc1ccc2c(-c3ccccc3)nc(=O)n(C(C)C)c2c1 10.1038/s41467-023-40064-9
2146 9874 67 None -123 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None -123 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None -123 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None -123 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None -123 15 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
5284550 48495 15 None -1513 16 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 48495 15 None -1513 16 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5210 40112 48 None -7 8 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1200765 40112 48 None -7 8 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1419 40112 48 None -7 8 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
1043 8363 14 None -128 23 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
149 8363 14 None -128 23 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
8223 8363 14 None -128 23 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL442 8363 14 None -128 23 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00696 8363 14 None -128 23 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
10133 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
145714624 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
4361 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
608 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL240597 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
DB06777 7697 78 None 1 4 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
2585 7590 103 None -512 34 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None -512 34 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None -512 34 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None -512 34 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None -512 34 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2136 9869 30 None -2 21 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 9869 30 None -2 21 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 9869 30 None -2 21 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 9869 30 None -2 21 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 9869 30 None -2 21 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
103 10925 61 None -323 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 10925 61 None -323 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 10925 61 None -323 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 10925 61 None -323 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 10925 61 None -323 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
65700 85035 28 None -9 8 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 85035 28 None -9 8 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
213 10625 55 None -177 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 10625 55 None -177 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 10625 55 None -177 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 10625 55 None -177 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 10625 55 None -177 22 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
68555 109889 21 None -79 7 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 7 1 5 2.6 CNCCc1ccc(OC(=O)C(C)C)c(OC(=O)C(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL307739 109889 21 None -79 7 Human 5.5 pAC50 = 5.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
2803 7742 58 None -6 14 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 7742 58 None -6 14 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 7742 58 None -6 14 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 7742 58 None -6 14 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 7742 58 None -6 14 Human 7.5 pAC50 = 7.5 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
47319 33237 35 None -1 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1360 33237 35 None -1 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
2407 10145 76 None -1122 17 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 10145 76 None -1122 17 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 10145 76 None -1122 17 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 10145 76 None -1122 17 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 10145 76 None -1122 17 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
4418 40996 85 None -19 18 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 40996 85 None -19 18 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
10531 8202 21 None -14 26 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None -14 26 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None -14 26 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None -14 26 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None -14 26 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
2333 149113 97 None -3 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
CHEMBL388590 149113 97 None -3 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
228 7233 28 None -724 19 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 7233 28 None -724 19 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 7233 28 None -724 19 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 7233 28 None -724 19 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 7233 28 None -724 19 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
3689 109548 55 None -549 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1372983 109548 55 None -549 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL305187 109548 55 None -549 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
2389 10104 118 None -95 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -95 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -95 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -95 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -95 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
2583 10548 118 None -2238 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 10548 118 None -2238 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 10548 118 None -2238 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 10548 118 None -2238 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 10548 118 None -2238 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
2220 9908 82 None -549 17 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 9908 82 None -549 17 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 9908 82 None -549 17 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 9908 82 None -549 17 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 9908 82 None -549 17 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
1960 9632 67 None -13 19 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 9632 67 None -13 19 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 9632 67 None -13 19 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 9632 67 None -13 19 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 9632 67 None -13 19 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
11079 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 9510 63 None -5 7 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
108000 63627 39 None -12 5 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
135418340 63627 39 None -12 5 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1643895 63627 39 None -12 5 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
47936 200201 88 None -91 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
CHEMBL52606 200201 88 None -91 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
2713 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 212050 82 None -8 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3294 8787 111 None -177 23 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -177 23 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -177 23 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -177 23 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -177 23 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2470 10425 50 None -69183 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 10425 50 None -69183 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 10425 50 None -69183 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 10425 50 None -69183 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 10425 50 None -69183 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
129211 10521 78 None -4265 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
2562 10521 78 None -4265 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
488 10521 78 None -4265 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
CHEMBL836 10521 78 None -4265 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
DB00706 10521 78 None -4265 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
213046 9164 59 None -35 17 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None -35 17 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None -35 17 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None -35 17 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None -35 17 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
2733 34586 112 None 1 3 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 0 1 2 1.8 O=c1[nH]c2cc(Cl)ccc2o1 10.1038/s41467-023-40064-9
CHEMBL1371 34586 112 None 1 3 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 169 0 1 2 1.8 O=c1[nH]c2cc(Cl)ccc2o1 10.1038/s41467-023-40064-9
1343 8670 62 None -3 12 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 8670 62 None -3 12 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 8670 62 None -3 12 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 8670 62 None -3 12 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 8670 62 None -3 12 Human 7.3 pAC50 = 7.3 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
135409453 10545 41 None -398 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None -398 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None -398 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
4011 89183 49 None -389 26 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 89183 49 None -389 26 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
2202 9906 96 None 16 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 9906 96 None 16 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 9906 96 None 16 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 9906 96 None 16 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 9906 96 None 16 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
212 10578 47 None -776 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -776 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -776 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -776 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -776 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
3658 10879 53 None -1 18 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 10879 53 None -1 18 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 10879 53 None -1 18 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 10879 53 None -1 18 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 10879 53 None -1 18 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
2467 74199 51 None -1 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
CHEMBL188921 74199 51 None -1 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
31101 7516 40 None -48 29 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None -48 29 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None -48 29 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None -48 29 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None -48 29 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
1890 9535 49 None -23 24 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None -23 24 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None -23 24 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None -23 24 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None -23 24 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
3926 214020 40 None -10 18 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 214020 40 None -10 18 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
25382 15929 37 None -181 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 15929 37 None -181 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
115 7131 71 None -123 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
2092 7131 71 None -123 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
7109 7131 71 None -123 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
CHEMBL709 7131 71 None -123 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
DB00346 7131 71 None -123 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
119570 9933 96 None -3019 10 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2233 9933 96 None -3019 10 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
953 9933 96 None -3019 10 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
CHEMBL301265 9933 96 None -3019 10 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
DB00413 9933 96 None -3019 10 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
445643 104164 69 None 1 7 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
CHEMBL269732 104164 69 None 1 7 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
11658860 9123 51 None -630 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 9123 51 None -630 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 9123 51 None -630 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 9123 51 None -630 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 9123 51 None -630 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
5311507 201594 41 None -645 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 201594 41 None -645 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
2342 7386 39 None -4 8 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
331 7386 39 None -4 8 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
7124 7386 39 None -4 8 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
CHEMBL1201250 7386 39 None -4 8 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
DB00767 7386 39 None -4 8 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
4640 85041 30 None -61 11 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2107011 85041 30 None -61 11 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
56959 38330 103 None -7 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1404 38330 103 None -7 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1526084 38330 103 None -7 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
46780481 114308 20 None -165 15 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 114308 20 None -165 15 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 114308 20 None -165 15 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 114308 20 None -165 15 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
118422671 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 9533 65 None -2691 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
104870 105656 47 None 1 10 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 105656 47 None 1 10 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 105656 47 None 1 10 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
1028 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 7079 71 None -10 19 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
2695 10613 81 None 2 6 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
5504 10613 81 None 2 6 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
7310 10613 81 None 2 6 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL770 10613 81 None 2 6 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00797 10613 81 None 2 6 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
2267 7347 71 None -35 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 7347 71 None -35 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 7347 71 None -35 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 7347 71 None -35 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 7347 71 None -35 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
1056 10144 116 None -15 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2405 10144 116 None -15 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
77999 10144 116 None -15 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
CHEMBL121 10144 116 None -15 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
DB00412 10144 116 None -15 10 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
54682461 91461 62 None -1 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 91461 62 None -1 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
12574 9383 88 None 1 8 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810 9383 88 None 1 8 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
CHEMBL19236 9383 88 None 1 8 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
DB09242 9383 88 None 1 8 Human 7.1 pAC50 = 7.1 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
135 9310 43 None -53 33 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -53 33 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -53 33 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -53 33 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -53 33 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1574 9093 12 None -3388 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
5359272 9093 12 None -3388 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
7595 9093 12 None -3388 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
CHEMBL592 9093 12 None -3388 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
DB00854 9093 12 None -3388 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
124 9755 47 None -3 25 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2032 9755 47 None -3 25 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636 9755 47 None -3 25 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL762 9755 47 None -3 25 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
DB00935 9755 47 None -3 25 Human 8.0 pAC50 = 8.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
180 7189 56 None -3890 38 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None -3890 38 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None -3890 38 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None -3890 38 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None -3890 38 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2169 51621 35 None -151 12 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 51621 35 None -151 12 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
5803 169006 84 None -2 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL41632 169006 84 None -2 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
1971 9641 38 None -3630 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 9641 38 None -3630 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 9641 38 None -3630 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 9641 38 None -3630 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 9641 38 None -3630 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2600 10551 74 None -416 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None -416 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None -416 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None -416 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None -416 32 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
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
40326 51895 68 None 1 2 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 6 0 3 6.1 CC1(C)C(C=C(Cl)Cl)C1C(=O)OCc1cccc(Oc2ccccc2)c1 10.1038/s41467-023-40064-9
CHEMBL1525 51895 68 None 1 2 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 6 0 3 6.1 CC1(C)C(C=C(Cl)Cl)C1C(=O)OCc1cccc(Oc2ccccc2)c1 10.1038/s41467-023-40064-9
2470 10425 50 None -69183 23 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 10425 50 None -69183 23 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 10425 50 None -69183 23 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 10425 50 None -69183 23 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 10425 50 None -69183 23 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
4993 129135 110 None -2 5 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL36 129135 110 None -2 5 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5365247 145207 33 None -69 10 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
CHEMBL37744 145207 33 None -69 10 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
2435 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
395 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
520 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
5386 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
CHEMBL844 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
DB00484 7509 100 None 7 10 Human 9.2 pEC50 = 9.2 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
521 8186 69 None -20 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
5311068 8186 69 None -20 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
835 8186 69 None -20 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
CHEMBL778 8186 69 None -20 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
DB00633 8186 69 None -20 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
2435 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
218362 211579 5 None 1 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL75030 211579 5 None 1 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
185076 193869 5 None 11 3 Human 8.9 pEC50 = 8.9 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL49137 193869 5 None 11 3 Human 8.9 pEC50 = 8.9 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
521 8186 69 None -20 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1016/j.bmc.2010.11.020
5311068 8186 69 None -20 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1016/j.bmc.2010.11.020
835 8186 69 None -20 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1016/j.bmc.2010.11.020
CHEMBL778 8186 69 None -20 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1016/j.bmc.2010.11.020
DB00633 8186 69 None -20 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1016/j.bmc.2010.11.020
44314198 111189 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL310335 111189 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
9815707 108246 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297752 108246 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
2803 7742 58 None -6 14 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 7742 58 None -6 14 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 7742 58 None -6 14 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 7742 58 None -6 14 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 7742 58 None -6 14 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
44292232 108098 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL296660 108098 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
11140345 210950 0 None -12 5 Human 7.0 pEC50 = 7 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 210950 0 None -12 5 Human 7.0 pEC50 = 7 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
24906200 199935 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
CHEMBL523048 199935 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
11211035 91778 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL223836 91778 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
11211035 91778 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL223836 91778 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
10382537 210945 12 None 4 2 Human 7.9 pEC50 = 7.9 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL70676 210945 12 None 4 2 Human 7.9 pEC50 = 7.9 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
44371864 57915 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 246 5 1 3 2.6 CCc1cccc(CC)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL157955 57915 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 246 5 1 3 2.6 CCc1cccc(CC)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
1960 9632 67 None -13 19 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2010.11.020
439260 9632 67 None -13 19 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2010.11.020
505 9632 67 None -13 19 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2010.11.020
CHEMBL1437 9632 67 None -13 19 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2010.11.020
DB00368 9632 67 None -13 19 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2010.11.020
44352207 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL128168 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
44352207 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL128168 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
44352207 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL128168 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
44352207 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL128168 25628 1 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
1960 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2011.11.025
439260 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2011.11.025
505 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2011.11.025
CHEMBL1437 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2011.11.025
DB00368 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2011.11.025
9859437 174801 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
CHEMBL432155 174801 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
1960 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2014.09.083
439260 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2014.09.083
505 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2014.09.083
CHEMBL1437 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2014.09.083
DB00368 9632 67 None -13 19 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2014.09.083
50994258 66863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 215 1 3 2 1.1 Cc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1641682 66863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 215 1 3 2 1.1 Cc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1739118 66863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 215 1 3 2 1.1 Cc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
53323136 63351 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 2 3 1.0 Clc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1641690 63351 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 2 3 1.0 Clc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
44312036 211344 1 None -19 2 Human 4.8 pEC50 = 4.8 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
CHEMBL72995 211344 1 None -19 2 Human 4.8 pEC50 = 4.8 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
24882007 19245 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.bmc.2010.11.020
CHEMBL1186220 19245 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.bmc.2010.11.020
56950526 78283 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 234 2 1 4 1.7 Clc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
CHEMBL1928323 78283 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 234 2 1 4 1.7 Clc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
CHEMBL1962709 78283 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 234 2 1 4 1.7 Clc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
57400570 78277 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 214 2 1 4 1.3 Cc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
CHEMBL1928322 78277 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 214 2 1 4 1.3 Cc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
CHEMBL1962686 78277 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 214 2 1 4 1.3 Cc1cccc2cnn(CC3=NCCN3)c12 10.1016/j.bmc.2011.11.025
44371755 55551 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 3 1 3 2.1 Cc1cccc(C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL155866 55551 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 3 1 3 2.1 Cc1cccc(C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
24882106 19338 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 2 3 1.0 Clc1cccc2c1cnn2N=C1NCCN1 10.1016/j.bmc.2010.11.020
CHEMBL1186774 19338 2 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 2 3 1.0 Clc1cccc2c1cnn2N=C1NCCN1 10.1016/j.bmc.2010.11.020
118717249 121903 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 1 2 3 0.5 Fc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.ejmech.2014.09.083
CHEMBL3343700 121903 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 1 2 3 0.5 Fc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.ejmech.2014.09.083
11098175 210949 0 None -186 4 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 210949 0 None -186 4 Human 6.7 pEC50 = 6.7 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
135399666 175542 7 None -23 6 Human 5.7 pEC50 = 5.7 Functional
Activity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assayActivity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assay
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 175542 7 None -23 6 Human 5.7 pEC50 = 5.7 Functional
Activity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assayActivity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assay
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
3086326 211310 22 None 13 3 Human 8.6 pEC50 = 8.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL72753 211310 22 None 13 3 Human 8.6 pEC50 = 8.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
131829 211506 15 None 37 3 Human 8.6 pEC50 = 8.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
CHEMBL74283 211506 15 None 37 3 Human 8.6 pEC50 = 8.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
44314200 109729 0 None -9 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
CHEMBL306377 109729 0 None -9 3 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
53324490 66866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1641681 66866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1739173 66866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2[nH]nc(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
10934575 211265 0 None -229 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 211265 0 None -229 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
11140347 211312 1 None -13 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 211312 1 None -13 5 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
11000184 19824 0 None -74 5 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 19824 0 None -74 5 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 19824 0 None -74 5 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
11173568 91416 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222371 91416 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
135453290 140384 33 None -1318 7 Human 5.6 pEC50 = 5.6 Functional
Activity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assayActivity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 140384 33 None -1318 7 Human 5.6 pEC50 = 5.6 Functional
Activity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assayActivity at adrenergic alpha2A receptor expressed in human clonic adenocarcinoma HT29 cell by tissue contraction assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
44449277 161962 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402388 161962 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
68712 107114 60 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
CHEMBL289480 107114 60 None 1 7 Human 6.6 pEC50 = 6.6 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
44312037 211398 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73392 211398 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
2803 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2010.11.020
516 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2010.11.020
704 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2010.11.020
CHEMBL134 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2010.11.020
DB00575 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2010.11.020
11043720 98947 0 None -257 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL242265 98947 0 None -257 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
11043720 98947 0 None -257 3 Human 4.5 pEC50 = 4.5 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL242265 98947 0 None -257 3 Human 4.5 pEC50 = 4.5 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
124 9755 47 None -3 25 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 9755 47 None -3 25 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 9755 47 None -3 25 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 9755 47 None -3 25 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 9755 47 None -3 25 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2803 7742 58 None -6 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2011.11.025
516 7742 58 None -6 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2011.11.025
704 7742 58 None -6 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2011.11.025
CHEMBL134 7742 58 None -6 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2011.11.025
DB00575 7742 58 None -6 14 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2011.11.025
2146 9874 67 None -123 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
485 9874 67 None -123 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
6041 9874 67 None -123 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
CHEMBL1215 9874 67 None -123 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
DB00388 9874 67 None -123 15 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
57402718 77964 2 None 3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956201 77964 2 None 3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
11265631 143187 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
CHEMBL373535 143187 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
11097789 109775 1 None -52 5 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 109775 1 None -52 5 Human 6.5 pEC50 = 6.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
11265631 143187 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
CHEMBL373535 143187 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
49836306 25347 0 None -31 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276247 25347 0 None -31 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
44449247 102189 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256984 102189 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
9817256 211017 0 None -251 2 Human 5.5 pEC50 = 5.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 211017 0 None -251 2 Human 5.5 pEC50 = 5.5 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
9971924 191005 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL48341 191005 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
44421258 91521 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL1204386 91521 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL222933 91521 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
24882019 19340 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 215 1 2 3 0.7 Cc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
CHEMBL1186788 19340 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 215 1 2 3 0.7 Cc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.bmc.2010.11.020
1960 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm0408215
439260 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm0408215
505 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm0408215
CHEMBL1437 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm0408215
DB00368 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm0408215
1960 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm901262f
439260 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm901262f
505 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm901262f
CHEMBL1437 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm901262f
DB00368 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm901262f
1960 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm800250z
439260 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm800250z
505 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm800250z
CHEMBL1437 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm800250z
DB00368 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm800250z
1960 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm061487a
439260 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm061487a
505 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm061487a
CHEMBL1437 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm061487a
DB00368 9632 67 None -13 19 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm061487a
294234 109670 3 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
CHEMBL305928 109670 3 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
118717248 121902 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 1 2 3 0.5 Fc1ccc2cnn(N=C3NCCN3)c2c1 10.1016/j.ejmech.2014.09.083
CHEMBL3343699 121902 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 219 1 2 3 0.5 Fc1ccc2cnn(N=C3NCCN3)c2c1 10.1016/j.ejmech.2014.09.083
11140033 27455 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL130884 27455 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
11108001 17644 2 None -7 5 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2aAgonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2a
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 17644 2 None -7 5 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2aAgonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2a
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 17644 2 None -7 5 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2aAgonist potency at Alpha-2A adrenergic receptor assayed in CHO cells expressing human alpha 2a
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
2435 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
395 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
520 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
5386 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
CHEMBL844 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
DB00484 7509 100 None 7 10 Human 8.4 pEC50 = 8.4 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
11360447 91776 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
CHEMBL223829 91776 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
10859076 20454 0 None -83 4 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 20454 0 None -83 4 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 20454 0 None -83 4 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2A adrenergic receptor expressed in CHO cellsAgonist potency at Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
44449276 102426 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257976 102426 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
11098175 210949 0 None -186 4 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 210949 0 None -186 4 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
57391904 78256 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 200 2 1 4 1.0 c1ccc2c(c1)cnn2CC1=NCCN1 10.1016/j.bmc.2011.11.025
CHEMBL1928316 78256 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 200 2 1 4 1.0 c1ccc2c(c1)cnn2CC1=NCCN1 10.1016/j.bmc.2011.11.025
CHEMBL1962472 78256 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation countingAgonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
ChEMBL 200 2 1 4 1.0 c1ccc2c(c1)cnn2CC1=NCCN1 10.1016/j.bmc.2011.11.025
44449691 102937 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL260576 102937 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
24906159 194184 12 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
CHEMBL493675 194184 12 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
57400959 77963 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 268 4 1 5 0.9 CC(Oc1ccccc1S(C)(=O)=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956200 77963 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 268 4 1 5 0.9 CC(Oc1ccccc1S(C)(=O)=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
11265631 143187 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
CHEMBL373535 143187 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
1593 9119 66 None 1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
30668 9119 66 None 1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
9868 9119 66 None 1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
CHEMBL17860 9119 66 None 1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
DB04948 9119 66 None 1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
11109088 210959 0 None -14 5 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 210959 0 None -14 5 Human 8.2 pEC50 = 8.2 Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.Agonist potency at Alpha-2A stably expressed in CHO cells.
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
57395731 77965 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 4 1 4 1.7 CC(=O)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956202 77965 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysisAgonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
ChEMBL 232 4 1 4 1.7 CC(=O)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
49836305 25348 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276248 25348 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
24906199 194444 15 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL495096 194444 15 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
44292386 108259 0 None -35 2 Human 7.2 pEC50 = 7.2 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297827 108259 0 None -35 2 Human 7.2 pEC50 = 7.2 Functional
Alpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMPAlpha-2A adrenergic receptor agonism measured as ability to inhibit forskolin-stimulated synthesis of cAMP
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
17804479 102435 19 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258007 102435 19 None -1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assayAgonist activity at human cloned adrenergic alpha-2A receptor expressed in CHOK1 cells by beta-lactamase reporter gene assay
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
50994260 66865 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2c(N=C3NCCN3)n[nH]c12 10.1016/j.bmc.2010.11.020
CHEMBL1641689 66865 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2c(N=C3NCCN3)n[nH]c12 10.1016/j.bmc.2010.11.020
CHEMBL1739136 66865 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 235 1 3 2 1.4 Clc1cccc2c(N=C3NCCN3)n[nH]c12 10.1016/j.bmc.2010.11.020
10333157 158017 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL396013 158017 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
10333157 158017 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL396013 158017 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulationAgonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
11371902 148416 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
CHEMBL385310 148416 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometryAgonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
11371902 148416 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL385310 148416 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
23622576 179551 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL451229 179551 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidificationAgonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
2803 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
516 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
704 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
CHEMBL134 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
DB00575 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphateAgonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
2803 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm100977d
516 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm100977d
704 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm100977d
CHEMBL134 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm100977d
DB00575 7742 58 None -6 14 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometryAgonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm100977d
10176999 110331 21 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
CHEMBL308570 110331 21 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Effective concentration at Alpha-2A adrenergic receptor from CHO-C10 cellsEffective concentration at Alpha-2A adrenergic receptor from CHO-C10 cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
53322686 66867 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 201 1 3 2 0.7 c1ccc2c(N=C3NCCN3)n[nH]c2c1 10.1016/j.bmc.2010.11.020
CHEMBL1641679 66867 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 201 1 3 2 0.7 c1ccc2c(N=C3NCCN3)n[nH]c2c1 10.1016/j.bmc.2010.11.020
CHEMBL1739201 66867 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 201 1 3 2 0.7 c1ccc2c(N=C3NCCN3)n[nH]c2c1 10.1016/j.bmc.2010.11.020
15675860 211208 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL72147 211208 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphateAlpha-2A adrenergic receptor agonistic potency as inhibition of forskolin-stimulated synthesis of cyclic adenosine monophosphate
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
2683 10606 60 None -1 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
5487 10606 60 None -1 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
7308 10606 60 None -1 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
CHEMBL1079 10606 60 None -1 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
DB00697 10606 60 None -1 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
24882007 19245 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.ejmech.2014.09.083
CHEMBL1186220 19245 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.ejmech.2014.09.083
132111 109772 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
CHEMBL306751 109772 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
132111 109772 5 None - 1 Human 5.9 pIC50 = 5.9 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
CHEMBL306751 109772 5 None - 1 Human 5.9 pIC50 = 5.9 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
123132228 163085 53 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against alpha2a adrenergic receptor (unknown origin)Antagonist activity against alpha2a adrenergic receptor (unknown origin)
ChEMBL 369 5 1 8 2.4 CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1 10.1021/acs.jmedchem.1c02148
CHEMBL4065484 163085 53 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against alpha2a adrenergic receptor (unknown origin)Antagonist activity against alpha2a adrenergic receptor (unknown origin)
ChEMBL 369 5 1 8 2.4 CS(=O)(=O)c1ccc(-c2cnc(NCc3ccco3)n3cnnc23)cc1 10.1021/acs.jmedchem.1c02148
11820372 20262 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 208 2 1 1 3.2 c1ccc2c(Cc3c[nH]cn3)cccc2c1 10.1021/jm00041a011
CHEMBL1193371 20262 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 208 2 1 1 3.2 c1ccc2c(Cc3c[nH]cn3)cccc2c1 10.1021/jm00041a011
CHEMBL544765 20262 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 208 2 1 1 3.2 c1ccc2c(Cc3c[nH]cn3)cccc2c1 10.1021/jm00041a011
68602 211905 80 None -10 4 Human 5.5 pIC50 = 5.5 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1021/jm00041a011
CHEMBL77921 211905 80 None -10 4 Human 5.5 pIC50 = 5.5 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1021/jm00041a011
10376336 19975 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 224 2 2 2 2.6 OC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
CHEMBL1191106 19975 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 224 2 2 2 2.6 OC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
CHEMBL542155 19975 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 224 2 2 2 2.6 OC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
132111 109772 5 None - 1 Human 5.0 pIC50 = 5.0 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
CHEMBL306751 109772 5 None - 1 Human 5.0 pIC50 = 5.0 Functional
Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.
ChEMBL 222 2 1 1 3.7 CC(c1c[nH]cn1)c1cccc2ccccc12 10.1021/jm00041a011
132256889 197226 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against alpha2a adrenergic receptor (unknown origin)Antagonist activity against alpha2a adrenergic receptor (unknown origin)
ChEMBL 378 5 1 7 3.6 COc1cccc(F)c1CNc1ccc(-c2cnc(C)nc2C)c2nncn12 10.1021/acs.jmedchem.1c02148
CHEMBL5178464 197226 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against alpha2a adrenergic receptor (unknown origin)Antagonist activity against alpha2a adrenergic receptor (unknown origin)
ChEMBL 378 5 1 7 3.6 COc1cccc(F)c1CNc1ccc(-c2cnc(C)nc2C)c2nncn12 10.1021/acs.jmedchem.1c02148
CHEMBL4755618 220820 39 None -1 2 Human 5.0 pIC50 = 5.0 Functional
Agonist activity at adrenergic receptor alpha2a (unknown origin)Agonist activity at adrenergic receptor alpha2a (unknown origin)
ChEMBL None None None Cc1ncccc1-c1cnc(NCc2c(F)ccc3c2CCO3)n2cnnc12 10.1021/acs.jmedchem.1c02148
13305910 18608 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 18608 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 18608 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 18608 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
16121006 18613 0 None - 0 Rat 5.9 pKd = 5.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182182 18613 0 None - 0 Rat 5.9 pKd = 5.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL217469 18613 0 None - 0 Rat 5.9 pKd = 5.9 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
499 10849 18 None - 1 Rat 6.6 pKd = 6.6 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
5685 10849 18 None - 1 Rat 6.6 pKd = 6.6 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
CHEMBL25554 10849 18 None - 1 Rat 6.6 pKd = 6.6 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
6603808 134300 3 None - 2 Rat 6.3 pKd = 6.3 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL214986 134300 3 None - 2 Rat 6.3 pKd = 6.3 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL36622 134300 3 None - 2 Rat 6.3 pKd = 6.3 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3740374 134300 3 None - 2 Rat 6.3 pKd = 6.3 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
44417713 19194 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1185884 19194 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL439346 19194 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@@H]1COc2ccccc2O1 10.1021/jm060358r
44324800 213727 0 None - 0 Human 9.1 pKi = 9.1 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL91157 213727 0 None - 0 Human 9.1 pKi = 9.1 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
44324972 170151 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL419316 170151 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
44579272 193874 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 499 7 0 9 4.3 c1ccc(Oc2ncccc2-c2noc(CN3CCCN(CC4COc5ccccc5O4)CC3)n2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL491420 193874 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 499 7 0 9 4.3 c1ccc(Oc2ncccc2-c2noc(CN3CCCN(CC4COc5ccccc5O4)CC3)n2)cc1 10.1016/j.bmcl.2008.08.055
10758200 70191 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 3 3.2 c1ccc(CN2CCN(CC3CCc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL179648 70191 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 3 3.2 c1ccc(CN2CCN(CC3CCc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
44579184 197732 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 340 4 0 5 2.7 COc1ccccc1N1CCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL518592 197732 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 340 4 0 5 2.7 COc1ccccc1N1CCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
44579271 193873 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 475 9 0 7 4.2 c1ccc(Oc2ncccc2COCCN2CCCN(CC3COc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL491419 193873 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 475 9 0 7 4.2 c1ccc(Oc2ncccc2COCCN2CCCN(CC3COc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
44579228 188433 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 467 7 2 7 2.9 CC(C)(C)Nc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL477608 188433 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 467 7 2 7 2.9 CC(C)(C)Nc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
44404321 77067 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 297 4 1 5 3.0 COc1cccc(N(NC2=NCCO2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
CHEMBL194323 77067 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 297 4 1 5 3.0 COc1cccc(N(NC2=NCCO2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
44579185 188593 1 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
CHEMBL477816 188593 1 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
44579230 188323 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 468 10 1 7 2.8 CCCCOc1cccc(C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)n1 10.1016/j.bmcl.2008.08.055
CHEMBL476569 188323 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 468 10 1 7 2.8 CCCCOc1cccc(C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)n1 10.1016/j.bmcl.2008.08.055
44324737 214017 0 None - 0 Human 8.3 pKi = 8.3 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL92860 214017 0 None - 0 Human 8.3 pKi = 8.3 Functional
Binding affinity for alpha-2A-adrenergic receptorBinding affinity for alpha-2A-adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
44579187 196458 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 513 8 1 8 3.3 N#Cc1cccc(Oc2ncccc2C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)c1 10.1016/j.bmcl.2008.08.055
CHEMBL515331 196458 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 513 8 1 8 3.3 N#Cc1cccc(Oc2ncccc2C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)c1 10.1016/j.bmcl.2008.08.055
44579229 196395 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 468 10 1 7 2.8 CCCCOc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL514837 196395 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPRAntagonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization by FLIPR
ChEMBL 468 10 1 7 2.8 CCCCOc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
2683 10606 60 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
5487 10606 60 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
7308 10606 60 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
CHEMBL1079 10606 60 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
DB00697 10606 60 None -1 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassayAgonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
Drug Central 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
1343 8670 62 None -3 12 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 8670 62 None -3 12 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 8670 62 None -3 12 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 8670 62 None -3 12 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 8670 62 None -3 12 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
2435 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 7509 100 None 7 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
521 8186 69 None -20 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
5311068 8186 69 None -20 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
835 8186 69 None -20 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
CHEMBL778 8186 69 None -20 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
DB00633 8186 69 None -20 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
523 10878 93 None -9 5 Human 5.7 pEC50 = 5.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
5707 10878 93 None -9 5 Human 5.7 pEC50 = 5.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
CHEMBL297362 10878 93 None -9 5 Human 5.7 pEC50 = 5.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
DB11477 10878 93 None -9 5 Human 5.7 pEC50 = 5.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
1960 9632 67 None -13 19 Human 6.7 pEC50 = 6.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
439260 9632 67 None -13 19 Human 6.7 pEC50 = 6.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
505 9632 67 None -13 19 Human 6.7 pEC50 = 6.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL1437 9632 67 None -13 19 Human 6.7 pEC50 = 6.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00368 9632 67 None -13 19 Human 6.7 pEC50 = 6.7 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
1028 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
139148732 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
479 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
5816 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL679 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00668 7079 71 None -10 19 Human 6.8 pEC50 = 6.8 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
1343 8670 62 None -3 12 Human 7.3 pEC50 = 7.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
3519 8670 62 None -3 12 Human 7.3 pEC50 = 7.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
522 8670 62 None -3 12 Human 7.3 pEC50 = 7.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
CHEMBL862 8670 62 None -3 12 Human 7.3 pEC50 = 7.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
DB01018 8670 62 None -3 12 Human 7.3 pEC50 = 7.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
2803 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
516 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
704 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
CHEMBL134 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
DB00575 7742 58 None -6 14 Human 7.6 pEC50 = 7.6 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
3952 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5353646 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5443 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5702063 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
CHEMBL1331786 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
CHEMBL420 8669 38 None -1 21 Human 8.3 pEC50 = 8.3 Functional
GTPγs bindingGTPγs binding
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
521 8186 69 None -20 5 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
5311068 8186 69 None -20 5 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
835 8186 69 None -20 5 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
CHEMBL778 8186 69 None -20 5 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
DB00633 8186 69 None -20 5 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
523 10878 93 None -9 5 Human 7.5 pEC50 = 7.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 10878 93 None -9 5 Human 7.5 pEC50 = 7.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 10878 93 None -9 5 Human 7.5 pEC50 = 7.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 10878 93 None -9 5 Human 7.5 pEC50 = 7.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
1960 9632 67 None -13 19 Human 7.7 pEC50 = 7.7 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 9632 67 None -13 19 Human 7.7 pEC50 = 7.7 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 9632 67 None -13 19 Human 7.7 pEC50 = 7.7 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 9632 67 None -13 19 Human 7.7 pEC50 = 7.7 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 9632 67 None -13 19 Human 7.7 pEC50 = 7.7 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
1028 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 7079 71 None -10 19 Human 8.0 pEC50 = 8 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
2683 10606 60 None -1 6 Human 8.4 pEC50 = 8.4 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
5487 10606 60 None -1 6 Human 8.4 pEC50 = 8.4 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
7308 10606 60 None -1 6 Human 8.4 pEC50 = 8.4 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
CHEMBL1079 10606 60 None -1 6 Human 8.4 pEC50 = 8.4 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
DB00697 10606 60 None -1 6 Human 8.4 pEC50 = 8.4 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
12574 9383 88 None 1 8 Human 8.5 pEC50 = 8.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 9383 88 None 1 8 Human 8.5 pEC50 = 8.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 9383 88 None 1 8 Human 8.5 pEC50 = 8.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 9383 88 None 1 8 Human 8.5 pEC50 = 8.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
2803 7742 58 None -6 14 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 7742 58 None -6 14 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 7742 58 None -6 14 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 7742 58 None -6 14 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 7742 58 None -6 14 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
1343 8670 62 None -3 12 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 8670 62 None -3 12 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 8670 62 None -3 12 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 8670 62 None -3 12 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 8670 62 None -3 12 Human 9.0 pEC50 = 9 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
2435 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 7509 100 None 7 10 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
3952 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 8669 38 None -1 21 Human 9.1 pEC50 = 9.1 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
521 8186 69 None -20 5 Human 9.5 pEC50 = 9.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 8186 69 None -20 5 Human 9.5 pEC50 = 9.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 8186 69 None -20 5 Human 9.5 pEC50 = 9.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 8186 69 None -20 5 Human 9.5 pEC50 = 9.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 8186 69 None -20 5 Human 9.5 pEC50 = 9.5 Functional
increased ERK1/2 phosphorylationincreased ERK1/2 phosphorylation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
523 10878 93 None -9 5 Human 5.1 pEC50 = 5.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 10878 93 None -9 5 Human 5.1 pEC50 = 5.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 10878 93 None -9 5 Human 5.1 pEC50 = 5.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 10878 93 None -9 5 Human 5.1 pEC50 = 5.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
1960 9632 67 None -13 19 Human 5.3 pEC50 = 5.3 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 9632 67 None -13 19 Human 5.3 pEC50 = 5.3 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 9632 67 None -13 19 Human 5.3 pEC50 = 5.3 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 9632 67 None -13 19 Human 5.3 pEC50 = 5.3 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 9632 67 None -13 19 Human 5.3 pEC50 = 5.3 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
1028 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 7079 71 None -10 19 Human 5.5 pEC50 = 5.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
12574 9383 88 None 1 8 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 9383 88 None 1 8 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 9383 88 None 1 8 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 9383 88 None 1 8 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
2683 10606 60 None -1 6 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
5487 10606 60 None -1 6 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
7308 10606 60 None -1 6 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
CHEMBL1079 10606 60 None -1 6 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
DB00697 10606 60 None -1 6 Human 5.8 pEC50 = 5.8 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
2803 7742 58 None -6 14 Human 6.4 pEC50 = 6.4 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 7742 58 None -6 14 Human 6.4 pEC50 = 6.4 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 7742 58 None -6 14 Human 6.4 pEC50 = 6.4 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 7742 58 None -6 14 Human 6.4 pEC50 = 6.4 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 7742 58 None -6 14 Human 6.4 pEC50 = 6.4 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
1343 8670 62 None -3 12 Human 6.5 pEC50 = 6.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 8670 62 None -3 12 Human 6.5 pEC50 = 6.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 8670 62 None -3 12 Human 6.5 pEC50 = 6.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 8670 62 None -3 12 Human 6.5 pEC50 = 6.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 8670 62 None -3 12 Human 6.5 pEC50 = 6.5 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
2142 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
4920903 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
502 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
5775 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
CHEMBL597 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
DB00692 9870 58 None -11 18 Human 7.1 pEC50 = 7.1 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 36101495
521 8186 69 None -20 5 Human 7.6 pEC50 = 7.6 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 8186 69 None -20 5 Human 7.6 pEC50 = 7.6 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 8186 69 None -20 5 Human 7.6 pEC50 = 7.6 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 8186 69 None -20 5 Human 7.6 pEC50 = 7.6 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 8186 69 None -20 5 Human 7.6 pEC50 = 7.6 Functional
increased cAMP generationincreased cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
2136 9869 30 None -2 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
4768 9869 30 None -2 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
7268 9869 30 None -2 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
CHEMBL753 9869 30 None -2 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
DB00925 9869 30 None -2 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
176 7186 66 None -1 40 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -1 40 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -1 40 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -1 40 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -1 40 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
1816 9318 102 None -39 12 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
4205 9318 102 None -39 12 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
7241 9318 102 None -39 12 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
CHEMBL654 9318 102 None -39 12 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
DB00370 9318 102 None -39 12 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10636247
3952 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 8669 38 None -1 21 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
1028 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 7079 71 None -10 19 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
523 10878 93 None -9 5 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 10878 93 None -9 5 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 10878 93 None -9 5 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 10878 93 None -9 5 Human 6.5 pIC50 = 6.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
1960 9632 67 None -13 19 Human 6.6 pIC50 = 6.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 9632 67 None -13 19 Human 6.6 pIC50 = 6.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 9632 67 None -13 19 Human 6.6 pIC50 = 6.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 9632 67 None -13 19 Human 6.6 pIC50 = 6.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 9632 67 None -13 19 Human 6.6 pIC50 = 6.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
12574 9383 88 None 1 8 Human 7.5 pIC50 = 7.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 9383 88 None 1 8 Human 7.5 pIC50 = 7.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 9383 88 None 1 8 Human 7.5 pIC50 = 7.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 9383 88 None 1 8 Human 7.5 pIC50 = 7.5 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
2683 10606 60 None -1 6 Human 7.6 pIC50 = 7.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
5487 10606 60 None -1 6 Human 7.6 pIC50 = 7.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
7308 10606 60 None -1 6 Human 7.6 pIC50 = 7.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
CHEMBL1079 10606 60 None -1 6 Human 7.6 pIC50 = 7.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
DB00697 10606 60 None -1 6 Human 7.6 pIC50 = 7.6 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
11079 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 9510 63 None -5 7 Human 7.8 pIC50 = 7.8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3952 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 8669 38 None -1 21 Human 7.9 pIC50 = 7.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
1343 8670 62 None -3 12 Human 8.0 pIC50 = 8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 8670 62 None -3 12 Human 8.0 pIC50 = 8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 8670 62 None -3 12 Human 8.0 pIC50 = 8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 8670 62 None -3 12 Human 8.0 pIC50 = 8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 8670 62 None -3 12 Human 8.0 pIC50 = 8 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3658 10879 53 None -1 18 Human 8.1 pIC50 = 8.1 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
517 10879 53 None -1 18 Human 8.1 pIC50 = 8.1 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
5709 10879 53 None -1 18 Human 8.1 pIC50 = 8.1 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
CHEMBL312448 10879 53 None -1 18 Human 8.1 pIC50 = 8.1 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
DB06694 10879 53 None -1 18 Human 8.1 pIC50 = 8.1 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
2803 7742 58 None -6 14 Human 8.2 pIC50 = 8.2 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 7742 58 None -6 14 Human 8.2 pIC50 = 8.2 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 7742 58 None -6 14 Human 8.2 pIC50 = 8.2 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 7742 58 None -6 14 Human 8.2 pIC50 = 8.2 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 7742 58 None -6 14 Human 8.2 pIC50 = 8.2 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
124 9755 47 None -3 25 Human 8.4 pIC50 = 8.4 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2032 9755 47 None -3 25 Human 8.4 pIC50 = 8.4 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
4636 9755 47 None -3 25 Human 8.4 pIC50 = 8.4 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
CHEMBL762 9755 47 None -3 25 Human 8.4 pIC50 = 8.4 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
DB00935 9755 47 None -3 25 Human 8.4 pIC50 = 8.4 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2435 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 7509 100 None 7 10 Human 8.9 pIC50 = 8.9 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
521 8186 69 None -20 5 Human 9.3 pIC50 = 9.3 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 8186 69 None -20 5 Human 9.3 pIC50 = 9.3 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 8186 69 None -20 5 Human 9.3 pIC50 = 9.3 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 8186 69 None -20 5 Human 9.3 pIC50 = 9.3 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 8186 69 None -20 5 Human 9.3 pIC50 = 9.3 Functional
inhibition of forskolin stimulated cAMP generationinhibition of forskolin stimulated cAMP generation
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495




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1353 8692 93 None -190 85 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -190 85 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -190 85 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -190 85 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -190 85 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
15387 52596 55 None -1 24 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1531134 52596 55 None -1 24 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
37 7565 60 None -3 17 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 7565 60 None -3 17 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 7565 60 None -3 17 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 7565 60 None -3 17 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 7565 60 None -3 17 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5591 164310 90 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
CHEMBL408 164310 90 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5022 8432 76 None - 9 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248 8432 76 None - 9 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
8182 8432 76 None - 9 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL231068 8432 76 None - 9 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
DB04908 8432 76 None - 9 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
176 7186 66 None -3 31 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 7186 66 None -3 31 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 7186 66 None -3 31 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 7186 66 None -3 31 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 7186 66 None -3 31 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
3152 195190 103 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 195190 103 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
2335 18620 22 None -5 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None -5 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None -5 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None -5 12 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
135 9310 43 None -4 56 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -4 56 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -4 56 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -4 56 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -4 56 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
98941 53724 17 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL154126 53724 17 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
103 10925 61 None -54 53 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 10925 61 None -54 53 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 10925 61 None -54 53 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 10925 61 None -54 53 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 10925 61 None -54 53 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
36811 8236 37 None - 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 8236 37 None - 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 8236 37 None - 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 8236 37 None - 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 8236 37 None - 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
5330286 74345 104 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
CHEMBL189963 74345 104 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
4908 195585 78 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 4 2.8 COc1cc(NC(C)CCCN)c2ncccc2c1 10.1038/s41467-023-40064-9
CHEMBL506 195585 78 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 4 2.8 COc1cc(NC(C)CCCN)c2ncccc2c1 10.1038/s41467-023-40064-9
1343 8670 62 None -11 9 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 8670 62 None -11 9 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 8670 62 None -11 9 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 8670 62 None -11 9 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 8670 62 None -11 9 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3351 101777 52 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
CHEMBL254857 101777 52 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
2389 10104 118 None -77 66 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -77 66 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -77 66 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -77 66 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -77 66 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5360696 8188 30 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
6953 8188 30 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
842 8188 30 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
CHEMBL52440 8188 30 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
DB00514 8188 30 None - 3 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
460612 212823 66 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
6918992 212823 66 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL852 212823 66 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
135398737 7745 93 None -26 90 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -26 90 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -26 90 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -26 90 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -26 90 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
21722 24764 31 None - 6 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 24764 31 None - 6 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
5351322 101566 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL25336 101566 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3584 10549 64 None -251 14 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 10549 64 None -251 14 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 10549 64 None -251 14 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 10549 64 None -251 14 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 10549 64 None -251 14 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
129893322 35391 56 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
4923 35391 56 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353897 35391 56 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
6178111 35391 56 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 2 5 2 2.2 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1377 35391 56 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
237 211644 48 None -1 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL546257 211644 48 None -1 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL554190 211644 48 None -1 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL7568 211644 48 None -1 13 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2402 10143 62 None -5 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 10143 62 None -5 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 10143 62 None -5 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 10143 62 None -5 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 10143 62 None -5 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
25295 20392 37 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1194287 20392 37 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
71698 210208 35 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 262 6 3 3 2.2 Cc1cc2c(OCC(O)CNC(C)C)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL65717 210208 35 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 262 6 3 3 2.2 Cc1cc2c(OCC(O)CNC(C)C)cccc2[nH]1 10.1038/s41467-023-40064-9
180 7189 56 None -58 40 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None -58 40 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None -58 40 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None -58 40 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None -58 40 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
5584 209990 44 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL644 209990 44 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
1400 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 8738 70 None - 3 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
4151 10379 89 None - 3 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 10379 89 None - 3 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 10379 89 None - 3 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 10379 89 None - 3 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 10379 89 None - 3 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
56959 38330 103 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1404 38330 103 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1526084 38330 103 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
46780481 114308 20 None -47 53 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 114308 20 None -47 53 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 114308 20 None -47 53 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 114308 20 None -47 53 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
1593 9119 66 None 5 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668 9119 66 None 5 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
9868 9119 66 None 5 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
CHEMBL17860 9119 66 None 5 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
DB04948 9119 66 None 5 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
1153 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
12668023 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026874 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026875 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
3341 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
6603851 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
933 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
939 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
985 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1160786 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1161520 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL588 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
DB00800 8409 58 None - 10 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
2683 10606 60 None -3 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487 10606 60 None -3 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
7308 10606 60 None -3 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
CHEMBL1079 10606 60 None -3 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
DB00697 10606 60 None -3 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
1909 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
2559 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
4474 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL1484 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL3302409 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
DB00622 9598 64 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3053 211913 95 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 393 16 5 8 -2.7 O=C(O)CN(CCN(CC(=O)O)CC(=O)O)CCN(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL780 211913 95 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
242 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
9853053 127297 74 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL354541 127297 74 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
93154 12208 29 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL107360 12208 29 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
68602 211905 80 None -1 8 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
CHEMBL77921 211905 80 None -1 8 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
5625 206447 72 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 10.1038/s41467-023-40064-9
CHEMBL593 206447 72 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 10.1038/s41467-023-40064-9
208898 72973 78 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
CHEMBL184412 72973 78 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3627 50903 18 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1515447 50903 18 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
2683 10606 60 None -3 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487 10606 60 None -3 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
7308 10606 60 None -3 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
CHEMBL1079 10606 60 None -3 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
DB00697 10606 60 None -3 4 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
3652 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
57 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
CHEMBL21536 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
DB15357 10869 79 None - 18 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
3354 48558 50 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
CHEMBL1493 48558 50 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
319 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 8106 44 None - 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
1343 8670 62 None -11 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 8670 62 None -11 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 8670 62 None -11 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 8670 62 None -11 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 8670 62 None -11 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
102 10899 48 None -5 49 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None -5 49 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None -5 49 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None -5 49 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None -5 49 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
242 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -26 51 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2540 11173 111 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 11173 111 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
1890 9535 49 None - 16 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None - 16 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None - 16 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None - 16 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None - 16 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1613 9127 53 None -8 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 9127 53 None -8 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 9127 53 None -8 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 9127 53 None -8 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 9127 53 None -8 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
9429 208912 58 None - 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 208912 58 None - 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
11057 182928 23 None -1 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
3468 182928 23 None -1 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL459265 182928 23 None -1 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL64894 182928 23 None -1 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3607 43156 72 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 339 12 1 3 4.7 CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 10.1038/s41467-023-40064-9
CHEMBL144673 43156 72 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 339 12 1 3 4.7 CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 10.1038/s41467-023-40064-9
16564 211774 32 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
CHEMBL76725 211774 32 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
21855 91021 42 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL22108 91021 42 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5472 212597 75 None -1 3 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 212597 75 None -1 3 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 212597 75 None -1 3 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
3152 195190 103 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 195190 103 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
10531 8202 21 None -5 24 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None -5 24 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None -5 24 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None -5 24 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None -5 24 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
68617 212306 62 None -3 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 212306 62 None -3 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 212306 62 None -3 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
1935 10506 97 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 10.1038/s41467-023-40064-9
2551 10506 97 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 10.1038/s41467-023-40064-9
6687 10506 97 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL95 10506 97 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 10.1038/s41467-023-40064-9
DB00382 10506 97 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2 10.1038/s41467-023-40064-9
213046 9164 59 None -19 9 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None -19 9 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None -19 9 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None -19 9 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None -19 9 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5314 210887 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 290 9 0 4 0.3 C[N+](C)(C)CCOC(=O)CCC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL703 210887 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 290 9 0 4 0.3 C[N+](C)(C)CCOC(=O)CCC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
7019 174755 106 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1308088 174755 106 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43184 174755 106 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
2470 10425 50 None - 58 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 10425 50 None - 58 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 10425 50 None - 58 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 10425 50 None - 58 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 10425 50 None - 58 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
25151352 147384 67 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 147384 67 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
68602 211905 80 None -1 8 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
CHEMBL77921 211905 80 None -1 8 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C 10.1038/s41467-023-40064-9
3634 90883 51 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL22077 90883 51 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
104903 63118 17 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 10.1038/s41467-023-40064-9
CHEMBL1630578 63118 17 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3294 8787 111 None -47 44 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -47 44 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -47 44 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -47 44 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -47 44 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3561 25849 39 None -1 11 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL1289 25849 39 None -1 11 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl 10.1038/s41467-023-40064-9
3157 8252 71 None -61 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 8252 71 None -61 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 8252 71 None -61 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 8252 71 None -61 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 8252 71 None -61 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
448537 167029 89 None -33 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 167029 89 None -33 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1547484 7727 74 None -5 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 7727 74 None -5 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 7727 74 None -5 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 7727 74 None -5 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 7727 74 None -5 20 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3047788 84971 15 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 3 0 2 3.3 CC1(CCN2CCCCC2)C(=O)CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2105148 84971 15 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 271 3 0 2 3.3 CC1(CCN2CCCCC2)C(=O)CCc2ccccc21 10.1038/s41467-023-40064-9
1212 8443 50 None -165 65 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 8443 50 None -165 65 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 8443 50 None -165 65 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 8443 50 None -165 65 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 8443 50 None -165 65 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1224 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 8214 83 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
135398737 7745 93 None -26 90 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -26 90 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -26 90 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -26 90 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -26 90 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
2585 7590 103 None -28 22 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None -28 22 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None -28 22 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None -28 22 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None -28 22 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1574 9093 12 None - 6 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
5359272 9093 12 None - 6 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
7595 9093 12 None - 6 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
CHEMBL592 9093 12 None - 6 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
DB00854 9093 12 None - 6 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 257 0 1 2 3.1 Oc1ccc2c(c1)[C@]13CCCC[C@H]3[C@@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
242 7258 124 None -26 51 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -26 51 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -26 51 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -26 51 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -26 51 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3678 101567 57 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL253371 101567 57 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
3002977 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
803 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
806 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1201187 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
CHEMBL256907 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
CHEMBL584744 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
DB04835 9238 71 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 513 8 1 5 6.0 O=C(C1CCC(CC1)(F)F)N[C@H](c1ccccc1)CCN1[C@@H]2CC[C@H]1CC(C2)n1c(C)nnc1C(C)C 10.1038/s41467-023-40064-9
441383 27105 57 None -2 17 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1306 27105 57 None -2 17 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
193962 110570 106 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 434 4 2 7 4.7 Cc1cc(C#N)cc(C)c1Oc1nc(Nc2ccc(C#N)cc2)nc(N)c1Br 10.1038/s41467-023-40064-9
CHEMBL308954 110570 106 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
23497 29664 38 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 3 3 5 0.1 COC(=O)[C@@H](N)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1328898 29664 38 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 3 3 5 0.1 COC(=O)[C@@H](N)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
11154555 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
5037 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
7671 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL2028019 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL3085826 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB06016 7587 62 None - 12 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2107 9829 50 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747 9829 50 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
9216 9829 50 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL251940 9829 50 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB01608 9829 50 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2580 85170 18 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL2110775 85170 18 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
2600 10551 74 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None - 13 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1599 9120 50 None - 16 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955 9120 50 None - 16 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7215 9120 50 None - 16 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL841 9120 50 None - 16 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00836 9120 50 None - 16 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3280 55223 28 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL1555736 55223 28 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
5440 35497 37 None - 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 35497 37 None - 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
72287 67835 38 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1764 67835 38 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5210 40112 48 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1200765 40112 48 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1419 40112 48 None - 4 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
213046 9164 59 None -19 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None -19 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None -19 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None -19 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None -19 9 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3601 21275 9 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1201349 21275 9 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
115368 9830 47 None - 4 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
2112 9830 47 None - 4 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
7556 9830 47 None - 4 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1472975 9830 47 None - 4 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
DB08922 9830 47 None - 4 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2148 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
2150 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
2784 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
5610 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
CHEMBL11608 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
DB08841 10662 114 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1038/s41467-023-40064-9
11079 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 9510 63 None -1 5 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
2162 48288 100 None 1 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 48288 100 None 1 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2146 9874 67 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
11434515 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11519741 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
4484 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
7449 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1194325 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
DB08897 7049 6 None - 5 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
2520 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2337 10030 77 None -50 62 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -50 62 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -50 62 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -50 62 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -50 62 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
2520 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 210787 70 None -6 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1531 9046 69 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1038/s41467-023-40064-9
3869 9046 69 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1038/s41467-023-40064-9
7207 9046 69 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1038/s41467-023-40064-9
CHEMBL429 9046 69 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1038/s41467-023-40064-9
DB00598 9046 69 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1038/s41467-023-40064-9
135398745 9688 112 None -93 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -93 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -93 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -93 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
60663 182448 42 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1421212 182448 42 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1534525 182448 42 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL45816 182448 42 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3598 194600 76 None -2 7 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL496 194600 76 None -2 7 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
228 7233 28 None -5 23 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 7233 28 None -5 23 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 7233 28 None -5 23 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 7233 28 None -5 23 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 7233 28 None -5 23 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2406 107180 89 None -16 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
CHEMBL290106 107180 89 None -16 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
135412795 51525 23 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 296 1 1 3 3.4 O=C1CN=C(c2ccccc2)c2c(sc3c2CCCC3)N1 10.1038/s41467-023-40064-9
CHEMBL1521495 51525 23 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 296 1 1 3 3.4 O=C1CN=C(c2ccccc2)c2c(sc3c2CCCC3)N1 10.1038/s41467-023-40064-9
3166 176199 23 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL442444 176199 23 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
134 9292 24 None -74 67 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 9292 24 None -74 67 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 9292 24 None -74 67 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 9292 24 None -74 67 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 9292 24 None -74 67 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2028 9753 80 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
359 9753 80 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
4634 9753 80 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
CHEMBL1231 9753 80 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
DB01062 9753 80 None - 11 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
124087 8171 114 None - 15 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 8171 114 None - 15 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 8171 114 None - 15 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 8171 114 None - 15 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 8171 114 None - 15 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
2343 21226 57 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 431 5 2 6 2.2 NS(=O)(=O)c1cc2c(cc1Cl)N=C(CSCc1ccccc1)NS2(=O)=O 10.1038/s41467-023-40064-9
CHEMBL1201039 21226 57 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 431 5 2 6 2.2 NS(=O)(=O)c1cc2c(cc1Cl)N=C(CSCc1ccccc1)NS2(=O)=O 10.1038/s41467-023-40064-9
82146 11302 113 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
CHEMBL1023 11302 113 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1027 8357 73 None - 2 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3241 8357 73 None - 2 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
7176 8357 73 None - 2 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL1106 8357 73 None - 2 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB00751 8357 73 None - 2 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2200 26975 61 None - 2 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 26975 61 None - 2 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 26975 61 None - 2 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
3675 14506 68 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 136 3 2 2 0.7 NNCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1089 14506 68 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 136 3 2 2 0.7 NNCCc1ccccc1 10.1038/s41467-023-40064-9
1712 9270 43 None - 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
4078 9270 43 None - 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
7227 9270 43 None - 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
CHEMBL1088 9270 43 None - 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
DB00933 9270 43 None - 22 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
1753 9282 28 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
483 9282 28 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
6082 9282 28 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
CHEMBL524 9282 28 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
DB00723 9282 28 None - 5 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
3157 8252 71 None -61 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 8252 71 None -61 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 8252 71 None -61 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 8252 71 None -61 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 8252 71 None -61 12 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2473 169962 47 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 248 5 2 4 1.7 CC(C)(C)NCC(O)COc1ccccc1C#N 10.1038/s41467-023-40064-9
CHEMBL418134 169962 47 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 248 5 2 4 1.7 CC(C)(C)NCC(O)COc1ccccc1C#N 10.1038/s41467-023-40064-9
2805 168669 38 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL415087 168669 38 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2303 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 9961 68 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
2966 65923 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 175 0 2 1 0.9 N=C(N)N1CCc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1593558 65923 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 175 0 2 1 0.9 N=C(N)N1CCc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL169901 65923 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 175 0 2 1 0.9 N=C(N)N1CCc2ccccc2C1 10.1038/s41467-023-40064-9
2286 9957 51 None -13 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 9957 51 None -13 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 9957 51 None -13 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 9957 51 None -13 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 9957 51 None -13 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL5291995 201315 0 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4418 40996 85 None - 7 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 40996 85 None - 7 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
3584 10549 64 None -251 14 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 10549 64 None -251 14 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 10549 64 None -251 14 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 10549 64 None -251 14 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 10549 64 None -251 14 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2200 26975 61 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 26975 61 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 26975 61 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
180 7189 56 None -58 40 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None -58 40 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None -58 40 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None -58 40 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None -58 40 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL4743867 220812 14 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
6237 93579 46 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 518 3 1 3 5.1 CCc1oc2ccccc2c1C(=O)c1cc(I)c(O)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL232201 93579 46 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1588 9105 27 None 1 44 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
28864 9105 27 None 1 44 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
43 9105 27 None 1 44 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL157138 9105 27 None 1 44 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB00589 9105 27 None 1 44 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
10531 8202 21 None -5 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None -5 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None -5 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None -5 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None -5 24 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
102 10899 48 None -5 49 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None -5 49 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None -5 49 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None -5 49 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None -5 49 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3658 10879 53 None -5 8 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 10879 53 None -5 8 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 10879 53 None -5 8 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 10879 53 None -5 8 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 10879 53 None -5 8 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
119584 9373 102 None -2 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1038/s41467-023-40064-9
1848 9373 102 None -2 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1038/s41467-023-40064-9
242 9373 102 None -2 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1038/s41467-023-40064-9
CHEMBL60889 9373 102 None -2 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1038/s41467-023-40064-9
DB11675 9373 102 None -2 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl 10.1038/s41467-023-40064-9
2803 7742 58 None -1 19 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 7742 58 None -1 19 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 7742 58 None -1 19 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 7742 58 None -1 19 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 7742 58 None -1 19 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
2342 7386 39 None -1 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
331 7386 39 None -1 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
7124 7386 39 None -1 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
CHEMBL1201250 7386 39 None -1 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
DB00767 7386 39 None -1 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
2762 10635 31 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5587 10635 31 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
7318 10635 31 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1241 10635 31 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
DB00792 10635 31 None - 2 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
135 9310 43 None -4 56 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -4 56 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -4 56 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -4 56 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -4 56 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2710 91083 31 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL22150 91083 31 None - 3 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
62867 9903 35 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
7557 9903 35 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL398880 9903 35 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01621 9903 35 None - 2 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2865 10915 73 None -64 53 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -64 53 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -64 53 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -64 53 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -64 53 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2726 7706 68 None -87 72 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 7706 68 None -87 72 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 7706 68 None -87 72 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 7706 68 None -87 72 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 7706 68 None -87 72 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
214 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None -75 30 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
12488 8438 56 None -6 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
941361 8438 56 None -6 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
CHEMBL30008 8438 56 None -6 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
DB04841 8438 56 None -6 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2389 10104 118 None -77 66 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -77 66 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -77 66 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -77 66 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -77 66 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
16351 109507 47 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 109507 47 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
6726 8063 51 None -10 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7151 8063 51 None -10 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
749 8063 51 None -10 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL648 8063 51 None -10 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB01176 8063 51 None -10 13 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
68712 107114 60 None -1 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
CHEMBL289480 107114 60 None -1 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
3950 196287 109 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 233 4 1 3 2.3 O=NN(CCCl)C(=O)NC1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL514 196287 109 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 233 4 1 3 2.3 O=NN(CCCl)C(=O)NC1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL3039583 217728 0 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
121515 205878 63 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 4 1 4 3.4 CC[C@H]1CN2CC[C@H]1C[C@H]2[C@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL588934 205878 63 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 4 1 4 3.4 CC[C@H]1CN2CC[C@H]1C[C@H]2[C@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
2398 7741 62 None -14 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 7741 62 None -14 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 7741 62 None -14 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 7741 62 None -14 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 7741 62 None -14 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
3033538 8101 39 None - 9 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
7155 8101 39 None - 9 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
781 8101 39 None - 9 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1201216 8101 39 None - 9 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
DB00298 8101 39 None - 9 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
CHEMBL508338 195745 0 None -6 6 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL None None None None 10.1038/s41467-023-40064-9
65863 21237 57 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1201196 21237 57 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
135398745 9688 112 None -93 65 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -93 65 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -93 65 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -93 65 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1816 9318 102 None -51 18 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 9318 102 None -51 18 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 9318 102 None -51 18 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 9318 102 None -51 18 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 9318 102 None -51 18 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
1548955 95356 20 None -1 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2800 95356 20 None -1 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL2355051 95356 20 None -1 18 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3547 148151 71 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL38380 148151 71 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL541388 148151 71 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
4735 201894 96 None -9 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL361506 201894 96 None -9 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL55 201894 96 None -9 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
12555 24733 53 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL12610 24733 53 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
6077 157477 31 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 157477 31 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4822 51806 47 None - 1 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL152408 51806 47 None - 1 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
34040 34858 72 None - 1 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
CHEMBL1372950 34858 72 None - 1 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4098 39279 30 None -13 11 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1255739 39279 30 None -13 11 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1411979 39279 30 None -13 11 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 10.1038/s41467-023-40064-9
16362 9899 71 None -501 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None -501 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None -501 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None -501 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None -501 29 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
9822750 85184 65 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL2111097 85184 65 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2142 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 9870 58 None -2 37 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
3783 20777 23 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 3 4 2.9 CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL1197051 20777 23 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
7029 20441 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 205 5 0 2 2.6 CCN(CC)C(C)C(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1194666 20441 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 205 5 0 2 2.6 CCN(CC)C(C)C(=O)c1ccccc1 10.1038/s41467-023-40064-9
71897 85023 19 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
CHEMBL2106537 85023 19 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2142 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 9870 58 None -2 37 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4209 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2993 121470 24 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL121663 121470 24 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL333826 121470 24 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2803 7742 58 None -1 19 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 7742 58 None -1 19 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 7742 58 None -1 19 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 7742 58 None -1 19 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 7742 58 None -1 19 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
2389 10104 118 None -77 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -77 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -77 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -77 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -77 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4167 21272 43 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL1201342 21272 43 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
4034 62596 55 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 62596 55 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
60860 212418 30 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL1615777 212418 30 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL818 212418 30 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
2446 161432 57 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 7 2 4 2.1 CCN(CC)CCNC(=O)c1cc(Br)c(N)cc1OC 10.1038/s41467-023-40064-9
CHEMBL399510 161432 57 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
277 8083 62 None -33 50 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913 8083 62 None -33 50 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
765 8083 62 None -33 50 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL516 8083 62 None -33 50 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB00434 8083 62 None -33 50 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2284 9956 33 None -12 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 9956 33 None -12 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 9956 33 None -12 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 9956 33 None -12 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 9956 33 None -12 29 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
3658 10879 53 None -5 8 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 10879 53 None -5 8 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 10879 53 None -5 8 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 10879 53 None -5 8 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 10879 53 None -5 8 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
1960 9632 67 None -23 26 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 9632 67 None -23 26 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 9632 67 None -23 26 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 9632 67 None -23 26 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 9632 67 None -23 26 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
102 10899 48 None -5 49 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None -5 49 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None -5 49 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None -5 49 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None -5 49 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
68802 116812 37 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
CHEMBL32350 116812 37 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
4209 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 9937 75 None -1380 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3158 63041 27 None -3467 20 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 63041 27 None -3467 20 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
11976 7707 59 None - 24 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 7707 59 None - 24 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 7707 59 None - 24 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 7707 59 None - 24 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
681 8247 72 None - 38 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
940 8247 72 None - 38 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
947 8247 72 None - 38 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL59 8247 72 None - 38 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00988 8247 72 None - 38 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
31101 7516 40 None -10 35 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None -10 35 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None -10 35 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None -10 35 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None -10 35 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
22530 62904 58 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1600878 62904 58 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1625607 62904 58 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
2510 10034 75 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@H]2[C@@H](c1ccnc2c1cc(OC)cc2)O 10.1038/s41467-023-40064-9
3034034 10034 75 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@H]2[C@@H](c1ccnc2c1cc(OC)cc2)O 10.1038/s41467-023-40064-9
4523 10034 75 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@H]2[C@@H](c1ccnc2c1cc(OC)cc2)O 10.1038/s41467-023-40064-9
CHEMBL170 10034 75 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@H]2[C@@H](c1ccnc2c1cc(OC)cc2)O 10.1038/s41467-023-40064-9
DB00468 10034 75 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@H]2[C@@H](c1ccnc2c1cc(OC)cc2)O 10.1038/s41467-023-40064-9
2181 9902 46 None -58 34 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
4830 9902 46 None -58 34 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
92 9902 46 None -58 34 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL440294 9902 46 None -58 34 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
DB09286 9902 46 None -58 34 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2391 214232 92 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 361 5 0 5 4.1 CC(=O)Oc1ccc(C(c2ccc(OC(C)=O)cc2)c2ccccn2)cc1 10.1038/s41467-023-40064-9
CHEMBL942 214232 92 None - 1 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 361 5 0 5 4.1 CC(=O)Oc1ccc(C(c2ccc(OC(C)=O)cc2)c2ccccn2)cc1 10.1038/s41467-023-40064-9
2337 10030 77 None -50 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -50 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -50 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -50 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -50 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
22323 22071 32 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9571037 22071 32 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1213553 22071 32 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
10180 105645 47 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL279014 105645 47 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
2220 9908 82 None - 14 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 9908 82 None - 14 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 9908 82 None - 14 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 9908 82 None - 14 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 9908 82 None - 14 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
1712095 202171 30 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 397 9 1 5 4.9 CCOc1ccc(/C=C2\NCCc3cc(OCC)c(OCC)cc32)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL551978 202171 30 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 397 9 1 5 4.9 CCOc1ccc(/C=C2\NCCc3cc(OCC)c(OCC)cc32)cc1OCC 10.1038/s41467-023-40064-9
3336 101776 30 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1405922 101776 30 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL254832 101776 30 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3158 63041 27 None -3467 20 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 63041 27 None -3467 20 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
5489013 64179 32 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 8 2 4 3.0 COc1cccc(C(=O)CCN[C@@H](C)[C@H](O)c2ccccc2)c1 10.1038/s41467-023-40064-9
CHEMBL1651913 64179 32 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2105 9828 37 None -13 32 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 9828 37 None -13 32 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 9828 37 None -13 32 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 9828 37 None -13 32 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 9828 37 None -13 32 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3294 8787 111 None -47 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -47 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -47 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -47 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -47 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5328940 106992 107 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2683 109665 25 None -12 16 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL305906 109665 25 None -12 16 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL334255 109665 25 None -12 16 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
4151 10379 89 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 10379 89 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 10379 89 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 10379 89 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 10379 89 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2247 7293 81 None -58 42 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 7293 81 None -58 42 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 7293 81 None -58 42 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 7293 81 None -58 42 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 7293 81 None -58 42 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2351 10059 64 None -9 21 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
2820 10059 64 None -9 21 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
5035 10059 64 None -9 21 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
CHEMBL81 10059 64 None -9 21 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
DB00481 10059 64 None -9 21 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
2146 9874 67 None - 9 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None - 9 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None - 9 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None - 9 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None - 9 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
443869 84916 45 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2103761 84916 45 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2605 10555 30 None - 10 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 10.1038/s41467-023-40064-9
36920 10555 30 None - 10 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 10.1038/s41467-023-40064-9
571 10555 30 None - 10 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL434200 10555 30 None - 10 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 10.1038/s41467-023-40064-9
DB13775 10555 30 None - 10 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C 10.1038/s41467-023-40064-9
5419 24832 57 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL1200413 24832 57 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL1266 24832 57 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
8249 66179 65 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1528839 66179 65 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL170988 66179 65 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
191 7191 98 None -41 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 7191 98 None -41 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 7191 98 None -41 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 7191 98 None -41 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 7191 98 None -41 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2286 9957 51 None -13 30 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 9957 51 None -13 30 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 9957 51 None -13 30 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 9957 51 None -13 30 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 9957 51 None -13 30 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5354 162435 21 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL404849 162435 21 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1086 8371 27 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290 8371 27 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
7181 8371 27 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
CHEMBL1206 8371 27 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
DB00392 8371 27 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
4829 206735 108 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 356 7 1 5 3.2 CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1038/s41467-023-40064-9
CHEMBL595 206735 108 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 356 7 1 5 3.2 CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1 10.1038/s41467-023-40064-9
1227 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
2331 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
3957 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
4992 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL511 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
DB06691 9267 43 None -91 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/s41467-023-40064-9
37 7565 60 None -3 17 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 7565 60 None -3 17 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 7565 60 None -3 17 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 7565 60 None -3 17 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 7565 60 None -3 17 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3584 10549 64 None -251 14 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 10549 64 None -251 14 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 10549 64 None -251 14 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 10549 64 None -251 14 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 10549 64 None -251 14 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
7099 202301 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 209 0 2 3 2.6 Nc1ccc2cc3ccc(N)cc3nc2c1 10.1038/s41467-023-40064-9
CHEMBL55400 202301 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 209 0 2 3 2.6 Nc1ccc2cc3ccc(N)cc3nc2c1 10.1038/s41467-023-40064-9
1782 9296 84 None -5 23 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 9296 84 None -5 23 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 9296 84 None -5 23 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 9296 84 None -5 23 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 9296 84 None -5 23 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
5311507 201594 41 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 201594 41 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
26987 7736 33 None -158 21 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 7736 33 None -158 21 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 7736 33 None -158 21 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 7736 33 None -158 21 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 7736 33 None -158 21 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
3103 48432 49 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1492 48432 49 None - 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
31101 7516 40 None -10 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None -10 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None -10 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None -10 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None -10 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
135 9310 43 None -4 56 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None -4 56 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None -4 56 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None -4 56 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None -4 56 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
40 8329 58 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
77993 8329 58 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
995 8329 58 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1510 8329 58 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
DB00216 8329 58 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1577 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
2537 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5355 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
5501 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
643497 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
688272 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
958 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
960 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL196677 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL26 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL267044 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB00391 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB16021 10475 110 None -3 20 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
212 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5328940 106992 107 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
54477 91428 36 None - 22 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
CHEMBL22242 91428 36 None - 22 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
5353853 24758 47 None -16 15 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9556529 24758 47 None -16 15 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1262 24758 47 None -16 15 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
43082 67057 37 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1742452 67057 37 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
129211 10521 78 None -120 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
2562 10521 78 None -120 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
488 10521 78 None -120 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
CHEMBL836 10521 78 None -120 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
DB00706 10521 78 None -120 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
3952 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5443 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL1331786 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL420 8669 38 None -3 12 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
11079 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 9510 63 None -1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3344 205097 57 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 3 1 3 1.8 O=C1NCC2(CCN(CCc3ccccc3)CC2)O1 10.1038/s41467-023-40064-9
CHEMBL576127 205097 57 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 260 3 1 3 1.8 O=C1NCC2(CCN(CCc3ccccc3)CC2)O1 10.1038/s41467-023-40064-9
6075 156887 42 None -11 16 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL395110 156887 42 None -11 16 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
73417116 161210 0 None - 1 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3989843 161210 0 None - 1 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1038/s41467-023-40064-9
65772 67177 8 None - 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 345 5 3 6 2.6 COc1cc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL174984 67177 8 None - 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4209 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 9937 75 None -1380 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2444 21250 26 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
CHEMBL1201245 21250 26 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
213 10625 55 None -10 43 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 10625 55 None -10 43 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 10625 55 None -10 43 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 10625 55 None -10 43 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 10625 55 None -10 43 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
27901 84982 22 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL2105458 84982 22 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
114948 67071 14 None - 3 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL1743263 67071 14 None - 3 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1353 8692 93 None -190 85 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -190 85 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -190 85 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -190 85 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -190 85 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1028 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 7079 71 None -48 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
9887712 174247 104 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 6 4 6 1.8 CCOc1ccc(Cc2cc([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)ccc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL429910 174247 104 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 408 6 4 6 1.8 CCOc1ccc(Cc2cc([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)ccc2Cl)cc1 10.1038/s41467-023-40064-9
133 9274 52 None -23 43 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
1723 9274 52 None -23 43 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
28693 9274 52 None -23 43 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
CHEMBL19215 9274 52 None -23 43 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
DB13520 9274 52 None -23 43 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
54758501 145845 58 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
CHEMBL3786343 145845 58 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2146 9874 67 None - 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 9874 67 None - 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 9874 67 None - 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 9874 67 None - 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 9874 67 None - 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
2865 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
1613 9127 53 None -8 44 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 9127 53 None -8 44 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 9127 53 None -8 44 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 9127 53 None -8 44 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 9127 53 None -8 44 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
68818 85043 28 None - 0 Human 8.0 pAC50 = 8.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 217 1 2 3 2.2 c1ccc2c(SC3=NCCN3)c[nH]c2c1 10.1038/s41467-023-40064-9
CHEMBL2107015 85043 28 None - 0 Human 8.0 pAC50 = 8.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 217 1 2 3 2.2 c1ccc2c(SC3=NCCN3)c[nH]c2c1 10.1038/s41467-023-40064-9
10219 195575 37 None -1 5 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL493439 195575 37 None -1 5 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 480 7 1 6 4.9 CC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1C[C@H]1NCCc2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL50588 195575 37 None -1 5 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2865 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -64 53 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
2749 7132 40 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574 7132 40 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7237 7132 40 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL829 7132 40 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01246 7132 40 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
5568 204279 29 None - 5 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
66069 204279 29 None - 5 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL1201102 204279 29 None - 5 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL570 204279 29 None - 5 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4567 16720 34 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 16720 34 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
9419 42696 35 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1442422 42696 35 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
1224 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 8214 83 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
1830 9368 44 None -14 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 9368 44 None -14 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 9368 44 None -14 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 9368 44 None -14 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 9368 44 None -14 28 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
9417 140290 54 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 140290 54 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 140290 54 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
37464 25993 26 None - 4 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1290 25993 26 None - 4 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components 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
4601 213526 35 None -2 17 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201023 213526 35 None -2 17 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL900 213526 35 None -2 17 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
104870 105656 47 None -2 21 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 105656 47 None -2 21 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 105656 47 None -2 21 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5205 84962 58 None - 0 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
CHEMBL2104895 84962 58 None - 0 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation countingBinding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
168295528 199810 0 None -11 20 Human 5.9 pEC50 = 5.9 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -11 20 Human 5.9 pEC50 = 5.9 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -11 20 Human 5.9 pEC50 = 5.9 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs 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
168294767 199798 0 None -11 20 Human 5.3 pEC50 = 5.3 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -11 20 Human 5.3 pEC50 = 5.3 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -11 20 Human 5.3 pEC50 = 5.3 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
102 10899 48 None -5 49 Human 8.1 pEC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
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 10.1021/np058114h
3659 10899 48 None -5 49 Human 8.1 pEC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
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 10.1021/np058114h
8969 10899 48 None -5 49 Human 8.1 pEC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
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 10.1021/np058114h
CHEMBL15245 10899 48 None -5 49 Human 8.1 pEC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
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 10.1021/np058114h
DB01392 10899 48 None -5 49 Human 8.1 pEC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
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 10.1021/np058114h
168290235 199747 0 None -40 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -40 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -40 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs 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
164612037 192156 0 None -11 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -11 20 Human 6.1 pEC50 = 6.1 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
44377036 126934 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL351483 126934 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44376984 62997 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 485 3 0 5 4.0 Cc1nc2ccc(I)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162682 62997 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 485 3 0 5 4.0 Cc1nc2ccc(I)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44376923 63201 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2cccc(C)n2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL163190 63201 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2cccc(C)n2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
22120332 62819 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 389 4 0 6 3.4 COc1cccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc12 10.1016/s0960-894x(99)00591-0
CHEMBL162490 62819 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 389 4 0 6 3.4 COc1cccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc12 10.1016/s0960-894x(99)00591-0
1588 9105 27 None 1 44 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None 1 44 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None 1 44 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None 1 44 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None 1 44 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44376954 62514 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 387 3 0 5 4.0 Cc1cc(C)n2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
CHEMBL162232 62514 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 387 3 0 5 4.0 Cc1cc(C)n2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
22120322 62695 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2c1 10.1016/s0960-894x(99)00591-0
CHEMBL162370 62695 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2c1 10.1016/s0960-894x(99)00591-0
44377200 64194 1 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 437 3 0 5 4.1 Cc1nc2ccc(Br)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165350 64194 1 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 437 3 0 5 4.1 Cc1nc2ccc(Br)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
3294 8787 111 None - 44 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
71360 8787 111 None - 44 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
87 8787 111 None - 44 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
CHEMBL14376 8787 111 None - 44 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
DB04946 8787 111 None - 44 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
44376958 64253 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
CHEMBL165796 64253 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1ccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1 10.1016/s0960-894x(99)00591-0
3682 196216 12 None - 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic alpha2 receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2013.03.016
CHEMBL1256784 196216 12 None - 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic alpha2 receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2013.03.016
CHEMBL513389 196216 12 None - 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic alpha2 receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2013.03.016
3045401 62833 32 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 359 3 0 5 3.4 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162501 62833 32 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 359 3 0 5 3.4 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44376993 63258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 427 3 0 5 4.7 Cc1nc2c(Cl)cc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL163247 63258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 427 3 0 5 4.7 Cc1nc2c(Cl)cc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44377035 126908 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2c(C)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL351200 126908 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 3 0 5 3.7 Cc1nc2c(C)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44376900 63042 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 375 3 1 6 3.1 Cc1nc2c(O)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162826 63042 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 375 3 1 6 3.1 Cc1nc2c(O)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
44377007 63922 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3c(Cl)cccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL164612 63922 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3c(Cl)cccc3c2C1 10.1016/s0960-894x(99)00591-0
10531 8202 21 None -5 24 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -5 24 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -5 24 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -5 24 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -5 24 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44376927 62411 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 461 3 0 5 5.0 Cc1nc2c(Cl)cc(C(F)(F)F)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL162147 62411 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 461 3 0 5 5.0 Cc1nc2c(Cl)cc(C(F)(F)F)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
9951544 64150 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 375 3 0 5 3.8 Cc1nc2ccccn2c(=O)c1CCN1CCc2sc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165181 64150 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 375 3 0 5 3.8 Cc1nc2ccccn2c(=O)c1CCN1CCc2sc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
107715 207724 22 None -6 20 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -6 20 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -6 20 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44376936 64248 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 4 0 5 3.7 Cc1nc2ccccn2c(=O)c1CCCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165776 64248 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 373 4 0 5 3.7 Cc1nc2ccccn2c(=O)c1CCCN1CCc2oc3ccccc3c2C1 10.1016/s0960-894x(99)00591-0
10095594 19140 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1185501 19140 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL417550 19140 0 None - 0 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10342423 106245 0 None - 1 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28312 106245 0 None - 1 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL48925 106245 0 None - 1 Bovine 7.0 pIC50 = 7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
44401591 75672 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL192266 75672 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
1220 6975 55 None - 44 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
31 6975 55 None - 44 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
7 6975 55 None - 44 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
CHEMBL56 6975 55 None - 44 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00038a007
10070029 172196 0 None - 1 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL423841 172196 0 None - 1 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54089 172196 0 None - 1 Bovine 6.0 pIC50 = 6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
59271992 124826 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of alpha-adrenoceptor 2A (unknown origin)Inhibition of alpha-adrenoceptor 2A (unknown origin)
ChEMBL 513 13 2 7 3.5 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2OC(=O)NCc2ccccc2)C(C)C)ccc1OC 10.1016/j.bmcl.2015.02.040
CHEMBL3403995 124826 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of alpha-adrenoceptor 2A (unknown origin)Inhibition of alpha-adrenoceptor 2A (unknown origin)
ChEMBL 513 13 2 7 3.5 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2OC(=O)NCc2ccccc2)C(C)C)ccc1OC 10.1016/j.bmcl.2015.02.040
2477 7532 59 None - 29 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
36 7532 59 None - 29 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
437 7532 59 None - 29 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL49 7532 59 None - 29 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
DB00490 7532 59 None - 29 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
121852 16938 7 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 16938 7 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 16938 7 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 102872 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 102872 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 102872 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10040815 103835 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL264027 103835 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26715 103835 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10047322 103915 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL26783 103915 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL50993 103915 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
10364722 105861 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 105861 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 105861 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10338595 169278 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL416747 169278 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10265863 200103 0 None - 0 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
CHEMBL52438 200103 0 None - 0 Bovine 5.0 pIC50 = 5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
14450375 171649 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 233 0 1 3 2.3 Cc1ccc(O)c2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
CHEMBL422024 171649 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 233 0 1 3 2.3 Cc1ccc(O)c2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
1305 7299 14 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 7299 14 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 7299 14 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
2585 7590 103 None -28 22 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -28 22 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -28 22 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -28 22 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -28 22 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
25208878 187842 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human adrenergic alpha2A receptorInhibition of human adrenergic alpha2A receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL475969 187842 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human adrenergic alpha2A receptorInhibition of human adrenergic alpha2A receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
44390778 71053 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL180962 71053 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
11284878 77216 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194602 77216 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
9885114 126382 5 None -95 12 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 126382 5 None -95 12 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL5070958 221028 3 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None NCCCCN(C[C@H]1Cc2ncccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acs.jmedchem.1c01564
4098 39279 30 None -13 11 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 39279 30 None -13 11 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 39279 30 None -13 11 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
2812 11551 101 None -32 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -32 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
16718919 206560 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human alpha-2a adrenergic receptorInhibition of human alpha-2a adrenergic receptor
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
CHEMBL593889 206560 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human alpha-2a adrenergic receptorInhibition of human alpha-2a adrenergic receptor
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
3561 25849 39 None -1 11 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 25849 39 None -1 11 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
23027211 204029 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 204029 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
11284878 71117 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181217 71117 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44390713 130473 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362193 130473 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401626 78129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195810 78129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL5076569 221228 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None NCCCCN(C[C@H]1Cc2cccnc2CN1)[C@H]1CCCc2cccnc21 10.1021/acs.jmedchem.1c01564
191 7191 98 None -41 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 7191 98 None -41 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 7191 98 None -41 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 7191 98 None -41 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 7191 98 None -41 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
100 10577 58 None -33 54 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -33 54 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -33 54 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -33 54 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -33 54 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
3158 63041 27 None -3467 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 63041 27 None -3467 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
1343 8670 62 None -11 9 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 8670 62 None -11 9 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 8670 62 None -11 9 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 8670 62 None -11 9 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 8670 62 None -11 9 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
4735 201894 96 None -9 10 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 201894 96 None -9 10 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 201894 96 None -9 10 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
3584 10549 64 None -251 14 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 10549 64 None -251 14 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 10549 64 None -251 14 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 10549 64 None -251 14 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 10549 64 None -251 14 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
44401552 172685 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL425012 172685 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
448537 167029 89 None -33 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 167029 89 None -33 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
2398 7741 62 None -14 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 7741 62 None -14 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 7741 62 None -14 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 7741 62 None -14 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 7741 62 None -14 29 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
15730 77893 80 None -2 10 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 77893 80 None -2 10 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
6075 156887 42 None -11 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 156887 42 None -11 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
31101 7516 40 None -10 35 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 7516 40 None -10 35 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 7516 40 None -10 35 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 7516 40 None -10 35 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 7516 40 None -10 35 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44390730 71091 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181099 71091 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44390742 130068 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL361442 130068 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
14450355 126746 0 None - 0 Bovine 6.8 pIC50 = 6.8 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 259 3 0 3 3.0 CCCN1CCC=C2c3c(OC)cccc3OCC21 10.1021/jm00123a039
CHEMBL349824 126746 0 None - 0 Bovine 6.8 pIC50 = 6.8 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 259 3 0 3 3.0 CCCN1CCC=C2c3c(OC)cccc3OCC21 10.1021/jm00123a039
6726 8063 51 None -10 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 8063 51 None -10 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 8063 51 None -10 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 8063 51 None -10 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 8063 51 None -10 13 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
150 9287 21 None -45 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 9287 21 None -45 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 9287 21 None -45 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 9287 21 None -45 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 9287 21 None -45 16 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
23027411 205299 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 205299 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
134 9292 24 None -74 67 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 9292 24 None -74 67 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 9292 24 None -74 67 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 9292 24 None -74 67 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 9292 24 None -74 67 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44190762 183659 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from adrenergic alpha2A receptorDisplacement of radioligand from adrenergic alpha2A receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 183659 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from adrenergic alpha2A receptorDisplacement of radioligand from adrenergic alpha2A 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
2750 210840 76 None -3 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -3 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
2351 10059 64 None -9 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -9 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -9 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -9 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -9 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
1042 8362 23 None -97 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 8362 23 None -97 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 8362 23 None -97 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 8362 23 None -97 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 8362 23 None -97 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2274 9947 58 None -10 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -10 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -10 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -10 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -10 31 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44390733 69268 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL178084 69268 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11342160 129713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360671 129713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11342160 129713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL360671 129713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
23027035 205326 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 205326 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
240 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 7731 43 None -12 25 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
26757 214757 31 None -1 2 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 nan
CHEMBL972 214757 31 None -1 2 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 nan
196129 74573 17 None -85 15 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 74573 17 None -85 15 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
4011 89183 49 None -35 24 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 89183 49 None -35 24 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
26987 7736 33 None -158 21 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 7736 33 None -158 21 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 7736 33 None -158 21 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 7736 33 None -158 21 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 7736 33 None -158 21 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
28417 46813 49 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
16215415 194111 1 None 3 5 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK912 from human cloned adrenergic alpha-2a receptorDisplacement of [3H]MK912 from human cloned adrenergic alpha-2a receptor
ChEMBL 471 9 2 3 3.8 CN(C)CCCOc1ccc(CCNC(=O)c2cc(Br)c[nH]2)cc1Br 10.1021/np800339e
CHEMBL493091 194111 1 None 3 5 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK912 from human cloned adrenergic alpha-2a receptorDisplacement of [3H]MK912 from human cloned adrenergic alpha-2a receptor
ChEMBL 471 9 2 3 3.8 CN(C)CCCOc1ccc(CCNC(=O)c2cc(Br)c[nH]2)cc1Br 10.1021/np800339e
10331436 7112 10 None - 6 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligandInhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 7112 10 None - 6 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligandInhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 7112 10 None - 6 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligandInhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
45482789 205704 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 205704 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A 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
1016 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -12 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
3823 56995 42 None -40 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 56995 42 None -40 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 56995 42 None -40 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
2803 7742 58 None - 19 Bovine 8.7 pIC50 = 8.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00123a039
516 7742 58 None - 19 Bovine 8.7 pIC50 = 8.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00123a039
704 7742 58 None - 19 Bovine 8.7 pIC50 = 8.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00123a039
CHEMBL134 7742 58 None - 19 Bovine 8.7 pIC50 = 8.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00123a039
DB00575 7742 58 None - 19 Bovine 8.7 pIC50 = 8.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00123a039
1043 8363 14 None -8 29 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -8 29 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -8 29 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -8 29 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -8 29 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44376975 62760 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 435 5 0 5 4.6 O=c1c(CCN2CCc3oc4ccccc4c3C2)c(Cc2ccccc2)nc2ccccn12 10.1016/s0960-894x(99)00591-0
CHEMBL162436 62760 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 435 5 0 5 4.6 O=c1c(CCN2CCc3oc4ccccc4c3C2)c(Cc2ccccc2)nc2ccccn12 10.1016/s0960-894x(99)00591-0
121852 16938 7 None - 1 Bovine 7.7 pIC50 = 7.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 16938 7 None - 1 Bovine 7.7 pIC50 = 7.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 16938 7 None - 1 Bovine 7.7 pIC50 = 7.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
135 9310 43 None -4 56 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 9310 43 None -4 56 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 9310 43 None -4 56 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 9310 43 None -4 56 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 9310 43 None -4 56 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
45485061 205533 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 205533 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44390787 129343 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360159 129343 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9981024 102872 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 102872 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 102872 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
131001 105769 7 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27995 105769 7 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
10321248 106202 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28287 106202 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50722 106202 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251673 106266 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283207 106266 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52396 106266 0 None - 1 Bovine 5.7 pIC50 = 5.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9978353 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL1178987 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL52785 18025 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
10105405 102807 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 233 5 0 2 3.1 CCCN(CCC)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL25984 102807 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 233 5 0 2 3.1 CCCN(CCC)C1COc2ccccc2C1 10.1021/jm00038a007
11743327 105478 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27763 105478 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
1577 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
2537 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
5355 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
5501 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
643497 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
688272 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
958 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
960 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL196677 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL26 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL267044 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
DB00391 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
DB16021 10475 110 None -3 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
657255 205863 34 None -10 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 205863 34 None -10 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
1210 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 7705 51 None -416 21 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
5467 212707 43 None -6 5 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC nan
CHEMBL84158 212707 43 None -6 5 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC nan
14151683 63311 0 None - 0 Bovine 6.7 pIC50 = 6.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 2 0 2 2.9 CCCN1CCC=C2c3ccccc3OCC21 10.1021/jm00123a039
CHEMBL163803 63311 0 None - 0 Bovine 6.7 pIC50 = 6.7 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 229 2 0 2 2.9 CCCN1CCC=C2c3ccccc3OCC21 10.1021/jm00123a039
44401616 76808 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193970 76808 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
45484995 205298 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 205298 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
5897 111988 80 None -7 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 111988 80 None -7 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
1212 8443 50 None -165 65 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -165 65 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -165 65 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -165 65 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -165 65 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
4601 213526 35 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 213526 35 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 213526 35 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
1530 8963 50 None -70 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 8963 50 None -70 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 8963 50 None -70 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 8963 50 None -70 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 8963 50 None -70 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
237 211644 48 None -1 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 211644 48 None -1 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 211644 48 None -1 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 211644 48 None -1 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
124 9755 47 None -4 32 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 9755 47 None -4 32 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 9755 47 None -4 32 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 9755 47 None -4 32 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 9755 47 None -4 32 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL5083458 221642 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None c1cnc2c(c1)CN[C@@H](CN(CCCCNC1COC1)[C@H]1CCCc3cccnc31)C2 10.1021/acs.jmedchem.1c01564
25014630 90314 1 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha2A adrenergic receptorInhibition of alpha2A adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 90314 1 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha2A adrenergic receptorInhibition of alpha2A adrenergic receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
2683 109665 25 None -12 16 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 109665 25 None -12 16 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 109665 25 None -12 16 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
14151624 62579 0 None - 0 Bovine 6.6 pIC50 = 6.6 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3ccc(O)cc3OC[C@H]21 10.1021/jm00123a039
CHEMBL162282 62579 0 None - 0 Bovine 6.6 pIC50 = 6.6 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3ccc(O)cc3OC[C@H]21 10.1021/jm00123a039
2337 10030 77 None -50 62 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 10030 77 None -50 62 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 10030 77 None -50 62 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 10030 77 None -50 62 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 10030 77 None -50 62 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
1305 7299 14 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
9934033 7299 14 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
CHEMBL182150 7299 14 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
4209 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 9937 75 None -1380 33 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
2105 9828 37 None -13 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 9828 37 None -13 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 9828 37 None -13 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 9828 37 None -13 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 9828 37 None -13 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
1782 9296 84 None -5 23 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 9296 84 None -5 23 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 9296 84 None -5 23 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 9296 84 None -5 23 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 9296 84 None -5 23 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
3151 8244 97 None -99 26 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 8244 97 None -99 26 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 8244 97 None -99 26 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 8244 97 None -99 26 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 8244 97 None -99 26 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
2803 7742 58 None -1 19 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 7742 58 None -1 19 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 7742 58 None -1 19 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 7742 58 None -1 19 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 7742 58 None -1 19 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
42 8844 57 None - 18 Bovine 5.6 pIC50 = 5.6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
56971 8844 57 None - 18 Bovine 5.6 pIC50 = 5.6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL8412 8844 57 None - 18 Bovine 5.6 pIC50 = 5.6 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL5077132 221263 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None CN(CCCCN(C[C@H]1Cc2ncccc2CN1)[C@H]1CCCc2cccnc21)C1CCOCC1 10.1021/acs.jmedchem.1c01564
277 8083 62 None -33 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 8083 62 None -33 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 8083 62 None -33 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 8083 62 None -33 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 8083 62 None -33 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
24180125 102431 71 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 469 5 2 8 3.7 O=C(Nc1ccccc1-c1cn2c(CN3CCNCC3)csc2n1)c1cnc2ccccc2n1 10.1021/jm8012954
CHEMBL257991 102431 71 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 469 5 2 8 3.7 O=C(Nc1ccccc1-c1cn2c(CN3CCNCC3)csc2n1)c1cnc2ccccc2n1 10.1021/jm8012954
68617 212306 62 None -3 26 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 212306 62 None -3 26 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 212306 62 None -3 26 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
3168 16034 92 None -123 22 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -123 22 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
1227 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 9267 43 None -91 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2435 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 7509 100 None -2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
44376845 62319 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 419 5 0 7 3.4 COc1cc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2cc1OC 10.1016/s0960-894x(99)00591-0
CHEMBL162058 62319 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 419 5 0 7 3.4 COc1cc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2cc1OC 10.1016/s0960-894x(99)00591-0
102 10899 48 None -5 49 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
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 10.1021/jm900458r
3659 10899 48 None -5 49 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
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 10.1021/jm900458r
8969 10899 48 None -5 49 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
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 10.1021/jm900458r
CHEMBL15245 10899 48 None -5 49 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
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 10.1021/jm900458r
DB01392 10899 48 None -5 49 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
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 10.1021/jm900458r
44377006 64237 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccc(Cl)cc3c2C1 10.1016/s0960-894x(99)00591-0
CHEMBL165677 64237 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccc(Cl)cc3c2C1 10.1016/s0960-894x(99)00591-0
10014217 106524 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
CHEMBL285010 106524 0 None - 1 Bovine 5.5 pIC50 = 5.5 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
10019102 39294 3 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 323 3 0 3 3.7 COC1Cc2ccccc2C2(CCN(Cc3ccccc3)CC2)O1 10.1021/jm010992z
CHEMBL141209 39294 3 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 323 3 0 3 3.7 COC1Cc2ccccc2C2(CCN(Cc3ccccc3)CC2)O1 10.1021/jm010992z
44390385 129294 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360117 129294 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
15987265 203666 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 203666 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
10915140 36247 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 351 5 0 3 4.2 COC1Cc2ccccc2C2(CCN(CCCc3ccccc3)CC2)O1 10.1021/jm010992z
CHEMBL138458 36247 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 351 5 0 3 4.2 COC1Cc2ccccc2C2(CCN(CCCc3ccccc3)CC2)O1 10.1021/jm010992z
2335 18620 22 None -5 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 18620 22 None -5 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 18620 22 None -5 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 18620 22 None -5 12 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
176 7186 66 None -3 31 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -3 31 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -3 31 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -3 31 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -3 31 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44596863 205706 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
ChEMBL 367 6 1 6 2.3 C=Cc1c(C)nn(CCCN2CCN(c3ccc(C)cc3)CC2)c(=O)c1N 10.1021/jm900458r
CHEMBL584606 205706 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 minsDisplacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
ChEMBL 367 6 1 6 2.3 C=Cc1c(C)nn(CCCN2CCN(c3ccc(C)cc3)CC2)c(=O)c1N 10.1021/jm900458r
2284 9956 33 None -12 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 9956 33 None -12 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 9956 33 None -12 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 9956 33 None -12 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 9956 33 None -12 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44390369 71384 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181727 71384 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
3038525 20321 114 None -2 3 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 435 3 0 5 5.5 O=c1ncn2nc(Sc3ccc(F)cc3F)ccc2c1-c1c(Cl)cccc1Cl nan
CHEMBL119385 20321 114 None -2 3 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 435 3 0 5 5.5 O=c1ncn2nc(Sc3ccc(F)cc3F)ccc2c1-c1c(Cl)cccc1Cl nan
44240743 13529 15 None - 1 Human 4.5 pIC50 = 4.5 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 370 7 2 3 4.3 O=C(NCCCCN1CCCCC1)Nc1ccc(-c2ccc(F)cc2)nc1 10.1021/jm901692q
CHEMBL1083787 13529 15 None - 1 Human 4.5 pIC50 = 4.5 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 370 7 2 3 4.3 O=C(NCCCCN1CCCCC1)Nc1ccc(-c2ccc(F)cc2)nc1 10.1021/jm901692q
180 7189 56 None -58 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 7189 56 None -58 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 7189 56 None -58 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 7189 56 None -58 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 7189 56 None -58 40 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2726 7706 68 None -87 72 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -87 72 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -87 72 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -87 72 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -87 72 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL1350036 74572 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1909062 74572 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
9807658 71320 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181466 71320 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
14151619 62189 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3c(O)cccc3OC[C@H]21 10.1021/jm00123a039
CHEMBL161947 62189 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3c(O)cccc3OC[C@H]21 10.1021/jm00123a039
2484 215072 71 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 nan
CHEMBL990 215072 71 None - 1 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 nan
119584 9373 102 None -2 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 9373 102 None -2 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 9373 102 None -2 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 9373 102 None -2 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 9373 102 None -2 6 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
57345320 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin)Inhibition of adrenergic alpha2A receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acsmedchemlett.8b00030
9882 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin)Inhibition of adrenergic alpha2A receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acsmedchemlett.8b00030
CHEMBL3091687 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin)Inhibition of adrenergic alpha2A receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acsmedchemlett.8b00030
57345320 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acs.jmedchem.1c01564
9882 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acs.jmedchem.1c01564
CHEMBL3091687 10604 9 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL 364 7 2 4 3.2 NCCCCN([C@H]1CCCc2c1nccc2)C[C@@H]1NCc2c(C1)cccc2 10.1021/acs.jmedchem.1c01564
9904205 212629 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 212629 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 212629 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 212629 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10219 195575 37 None -1 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL493439 195575 37 None -1 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL50588 195575 37 None -1 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
5472 212597 75 None -1 3 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL1717 212597 75 None -1 3 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL833 212597 75 None -1 3 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
2406 107180 89 None -16 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 107180 89 None -16 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
14151652 103415 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 261 3 1 3 3.1 CCCCN1CCC[C@@H]2c3cccc(O)c3OC[C@H]21 10.1021/jm00123a039
CHEMBL263574 103415 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 261 3 1 3 3.1 CCCCN1CCC[C@@H]2c3cccc(O)c3OC[C@H]21 10.1021/jm00123a039
10231050 71108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181184 71108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
1836 9370 59 None -43 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 9370 59 None -43 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 9370 59 None -43 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 9370 59 None -43 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 9370 59 None -43 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
4189 213701 96 None -18 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -18 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -18 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10024943 104165 0 None - 1 Bovine 6.4 pIC50 = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26975 104165 0 None - 1 Bovine 6.4 pIC50 = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52485 104165 0 None - 1 Bovine 6.4 pIC50 = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10429859 18814 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL1183429 18814 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL296395 18814 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
10092409 18818 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1183479 18818 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL299561 18818 0 None - 0 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10319624 105763 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27991 105763 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL298534 105763 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 106335 8 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 106335 8 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9975915 106512 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL284912 106512 0 None - 1 Bovine 5.4 pIC50 = 5.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10072866 204254 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51561 204254 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL56990 204254 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
5318 22348 49 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 22348 49 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 22348 49 None -1 13 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
5353853 24758 47 None -16 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -16 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -16 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
3952 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 8669 38 None -3 12 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
135 9310 43 None -4 56 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 9310 43 None -4 56 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 9310 43 None -4 56 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 9310 43 None -4 56 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 9310 43 None -4 56 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
10660 21188 58 None -43 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 21188 58 None -43 12 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
6918276 22383 7 None -16 8 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 22383 7 None -16 8 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
3198 212292 76 None -19 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -19 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -19 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
19426635 212372 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 212372 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
44390456 71675 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
CHEMBL182235 71675 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
1547484 7727 74 None -5 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 7727 74 None -5 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 7727 74 None -5 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 7727 74 None -5 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 7727 74 None -5 20 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL1441214 46591 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1476898 46591 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
44390715 130598 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362400 130598 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11204090 76611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193771 76611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
23027527 203571 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 203571 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
10381889 113846 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 113846 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 113846 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 113846 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
5198 26205 54 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 nan
CHEMBL12948 26205 54 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 nan
2247 7293 81 None -58 42 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -58 42 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -58 42 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -58 42 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -58 42 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
3117 214620 103 None -2 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
1353 8692 93 None -190 85 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -190 85 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -190 85 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -190 85 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -190 85 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
44401671 77041 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194173 77041 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
9980269 105859 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280586 105859 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54266 105859 0 None - 1 Bovine 6.3 pIC50 = 6.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251234 18017 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 18017 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 18017 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10476735 20503 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1195096 20503 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL553833 20503 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364722 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 105861 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
44318454 212788 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 212788 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human cloned Alpha-2A adrenergic receptorBinding affinity for human cloned Alpha-2A adrenergic receptor
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
14450361 62847 0 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 275 3 0 3 3.4 CCCN1CCC[C@@H]2c3c(OC)cc(C)cc3OC[C@H]21 10.1021/jm00123a039
CHEMBL162510 62847 0 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 275 3 0 3 3.4 CCCN1CCC[C@@H]2c3c(OC)cc(C)cc3OC[C@H]21 10.1021/jm00123a039
44390752 129774 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360876 129774 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL508338 195745 0 None -6 6 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
11057 182928 23 None -1 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 182928 23 None -1 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 182928 23 None -1 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 182928 23 None -1 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
135398745 9688 112 None -93 65 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -93 65 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -93 65 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -93 65 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1201549 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 7384 24 None -33 20 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
3598 194600 76 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 194600 76 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
10243700 63057 1 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm00123a039
CHEMBL162955 63057 1 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm00123a039
11204090 70281 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL180003 70281 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401449 77869 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195346 77869 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
10303307 71250 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181393 71250 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
1549008 212459 85 None - 1 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 nan
CHEMBL822 212459 85 None - 1 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 nan
2520 210787 70 None -6 12 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 210787 70 None -6 12 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 210787 70 None -6 12 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
133 9274 52 None -23 43 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -23 43 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -23 43 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -23 43 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -23 43 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44401508 76596 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL193666 76596 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
45485062 203947 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 203947 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
12488 8438 56 None -6 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 8438 56 None -6 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 8438 56 None -6 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 8438 56 None -6 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
CHEMBL1200633 215379 3 None -7 8 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
145949343 169711 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin)Inhibition of adrenergic alpha2A receptor (unknown origin)
ChEMBL 404 6 2 4 3.9 c1ccc2c(c1)CN[C@@H](CN(CC[C@H]1CCCNC1)[C@H]1CCCc3cccnc31)C2 10.1021/acsmedchemlett.8b00030
CHEMBL4174290 169711 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin)Inhibition of adrenergic alpha2A receptor (unknown origin)
ChEMBL 404 6 2 4 3.9 c1ccc2c(c1)CN[C@@H](CN(CC[C@H]1CCCNC1)[C@H]1CCCc3cccnc31)C2 10.1021/acsmedchemlett.8b00030
2142 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 9870 58 None -2 37 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
102 10899 48 None -5 49 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
3659 10899 48 None -5 49 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
8969 10899 48 None -5 49 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL15245 10899 48 None -5 49 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
DB01392 10899 48 None -5 49 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
73453 36389 24 None -3 17 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 36389 24 None -3 17 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44390710 71363 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181632 71363 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10252000 105323 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27650 105323 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50188 105323 0 None - 1 Bovine 5.2 pIC50 = 5.2 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
2162 48288 100 None 1 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 48288 100 None 1 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL5082142 221566 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None c1cnc2c(c1)CN[C@@H](CN(CCCCN1CCOCC1)[C@H]1CCCc3cccnc31)C2 10.1021/acs.jmedchem.1c01564
10357986 36678 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 309 3 0 3 3.9 COC1OC2(CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm010992z
CHEMBL138809 36678 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of idazoxane binding to noradrenaline alpha-2 receptorInhibition of idazoxane binding to noradrenaline alpha-2 receptor
ChEMBL 309 3 0 3 3.9 COC1OC2(CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm010992z
11080 35858 79 None 1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 35858 79 None 1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
44390706 128811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL359510 128811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
14151702 63120 1 None - 0 Bovine 6.2 pIC50 = 6.2 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 245 2 1 3 2.7 CCCN1CCC=C2c3cc(O)ccc3OCC21 10.1021/jm00123a039
CHEMBL163061 63120 1 None - 0 Bovine 6.2 pIC50 = 6.2 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 245 2 1 3 2.7 CCCN1CCC=C2c3cc(O)ccc3OCC21 10.1021/jm00123a039
6761 74574 19 None -6 18 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 74574 19 None -6 18 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
1752 52535 59 None -2 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
CHEMBL153062 52535 59 None -2 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
2286 9957 51 None -13 30 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 9957 51 None -13 30 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 9957 51 None -13 30 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 9957 51 None -13 30 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 9957 51 None -13 30 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL1458880 44624 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
9895868 19671 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL1188966 19671 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL537846 19671 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9895868 76357 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 76357 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
134551 7146 27 None -3 21 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -3 21 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -3 21 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -3 21 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
16718917 188461 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human adrenergic alpha2A receptorInhibition of human adrenergic alpha2A receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 188461 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human adrenergic alpha2A receptorInhibition of human adrenergic alpha2A receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
168281847 197815 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NECA from A2AAR in rat striatal membrane assessed as inhibition constant by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striatal membrane assessed as inhibition constant by radioligand competitive binding assay
ChEMBL 310 3 1 4 3.6 COc1ccc(/C=C2\CCc3c(O)cccc3C2=O)cc1OC 10.1016/j.ejmech.2021.113964
CHEMBL5187030 197815 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NECA from A2AAR in rat striatal membrane assessed as inhibition constant by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striatal membrane assessed as inhibition constant by radioligand competitive binding assay
ChEMBL 310 3 1 4 3.6 COc1ccc(/C=C2\CCc3c(O)cccc3C2=O)cc1OC 10.1016/j.ejmech.2021.113964
14151613 63264 0 None - 0 Bovine 7.2 pIC50 = 7.2 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 261 3 0 3 3.0 CCCN1CCC[C@@H]2c3c(OC)cccc3OC[C@H]21 10.1021/jm00123a039
CHEMBL163281 63264 0 None - 0 Bovine 7.2 pIC50 = 7.2 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 261 3 0 3 3.0 CCCN1CCC[C@@H]2c3c(OC)cccc3OC[C@H]21 10.1021/jm00123a039
44390726 129182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL360081 129182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
23027245 203907 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 203907 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]MK-912 from human adrenergic alpha2A receptorDisplacement of [3H]MK-912 from human adrenergic alpha2A receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
1971 9641 38 None -8 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 9641 38 None -8 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 9641 38 None -8 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 9641 38 None -8 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 9641 38 None -8 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4211 64596 83 None -1 4 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 64596 83 None -1 4 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
1028 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 7079 71 None -48 30 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
44390750 70252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL179878 70252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
14151647 62437 1 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3cccc(O)c3OC[C@H]21 10.1021/jm00123a039
CHEMBL162170 62437 1 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 2 1 3 2.7 CCCN1CCC[C@@H]2c3cccc(O)c3OC[C@H]21 10.1021/jm00123a039
3082597 106335 8 None - 1 Bovine 6.1 pIC50 = 6.1 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 106335 8 None - 1 Bovine 6.1 pIC50 = 6.1 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
12575 8769 30 None -5 17 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
54459 8769 30 None -5 17 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
CHEMBL10316 8769 30 None -5 17 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/s0960-894x(99)00591-0
102 10899 48 None -5 49 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
3659 10899 48 None -5 49 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
8969 10899 48 None -5 49 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
CHEMBL15245 10899 48 None -5 49 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
DB01392 10899 48 None -5 49 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
118112300 162773 18 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at alpha2A-adrenergic receptor (unknown origin)Antagonist activity at alpha2A-adrenergic receptor (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
CHEMBL4061793 162773 18 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at alpha2A-adrenergic receptor (unknown origin)Antagonist activity at alpha2A-adrenergic receptor (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
CHEMBL5093818 222224 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of alpha 2A adrenergic receptor (unknown origin)Inhibition of alpha 2A adrenergic receptor (unknown origin)
ChEMBL None None None CN(CCCCN(C[C@H]1Cc2ncccc2CN1)[C@H]1CCCc2cccnc21)C1CCC(F)(F)CC1 10.1021/acs.jmedchem.1c01564
3191 109635 97 None -8 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -8 25 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
1816 9318 102 None -51 18 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
4205 9318 102 None -51 18 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
7241 9318 102 None -51 18 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
CHEMBL654 9318 102 None -51 18 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
DB00370 9318 102 None -51 18 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1016/s0960-894x(99)00591-0
44401460 77682 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 391 7 2 6 2.5 CN(C)c1nc(NCC2CCC(CNS(C)(=O)=O)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL195123 77682 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 391 7 2 6 2.5 CN(C)c1nc(NCC2CCC(CNS(C)(=O)=O)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
14151595 63285 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 231 2 0 2 3.0 CCCN1CCC[C@@H]2c3ccccc3OC[C@H]21 10.1021/jm00123a039
CHEMBL163532 63285 0 None - 0 Bovine 7.1 pIC50 = 7.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 231 2 0 2 3.0 CCCN1CCC[C@@H]2c3ccccc3OC[C@H]21 10.1021/jm00123a039
70788951 33928 1 None -1 5 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1366 33928 1 None -1 5 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
46227396 208419 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human alpha-2a adrenergic receptorInhibition of human alpha-2a adrenergic receptor
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 208419 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human alpha-2a adrenergic receptorInhibition of human alpha-2a adrenergic receptor
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
42636941 185728 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]RX821002 form human recombinant alpha2A adrenergic receptorDisplacement of [3H]RX821002 form human recombinant alpha2A adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 185728 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]RX821002 form human recombinant alpha2A adrenergic receptorDisplacement of [3H]RX821002 form human recombinant alpha2A adrenergic receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
8447 195728 84 None -4 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 195728 84 None -4 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
2389 10104 118 None -77 66 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 10104 118 None -77 66 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 10104 118 None -77 66 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 10104 118 None -77 66 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 10104 118 None -77 66 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
44390499 136435 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367355 136435 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
135398737 7745 93 None -26 90 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 7745 93 None -26 90 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 7745 93 None -26 90 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 7745 93 None -26 90 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 7745 93 None -26 90 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
213 10625 55 None -10 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 10625 55 None -10 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 10625 55 None -10 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 10625 55 None -10 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 10625 55 None -10 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
3082597 106335 8 None - 1 Bovine 5.0 pIC50 = 5.0 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 106335 8 None - 1 Bovine 5.0 pIC50 = 5.0 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
36324 33896 76 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 293 4 0 2 4.9 Cc1ccc(/N=C/N(C)/C=N/c2ccc(C)cc2C)c(C)c1 nan
CHEMBL1365675 33896 76 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 293 4 0 2 4.9 Cc1ccc(/N=C/N(C)/C=N/c2ccc(C)cc2C)c(C)c1 nan
1548953 214458 27 None -1 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 214458 27 None -1 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
14450364 62777 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 1 0 3 2.6 COc1cc(C)cc2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
CHEMBL162449 62777 0 None - 0 Bovine 6.0 pIC50 = 6.0 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor at 1 uM
ChEMBL 247 1 0 3 2.6 COc1cc(C)cc2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
44390768 71248 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181383 71248 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cellsInhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
1562 7686 13 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
5312114 7686 13 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL17645 7686 13 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL195380 7686 13 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
441383 27105 57 None -2 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -2 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
164612037 192156 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 199747 0 None -40 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -40 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -40 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 199798 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 199810 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -11 20 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]RX821002 from human alpha-2A adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs 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
118714540 121289 0 None 5 4 Human 9.0 pKd = 9.0 Binding
Displacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from human adenosine A2a receptor K150A mutant expressed in COS-7 cells assessed as radioligand Kd compound preincubated for 30 minsDisplacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from human adenosine A2a receptor K150A mutant expressed in COS-7 cells assessed as radioligand Kd compound preincubated for 30 mins
ChEMBL 677 13 6 15 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(CCC(=O)Nc5ccc(OC(C)=O)c([N+](=O)[O-])c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/ml5002486
CHEMBL3335523 121289 0 None 5 4 Human 9.0 pKd = 9.0 Binding
Displacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from human adenosine A2a receptor K150A mutant expressed in COS-7 cells assessed as radioligand Kd compound preincubated for 30 minsDisplacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from human adenosine A2a receptor K150A mutant expressed in COS-7 cells assessed as radioligand Kd compound preincubated for 30 mins
ChEMBL 677 13 6 15 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(CCC(=O)Nc5ccc(OC(C)=O)c([N+](=O)[O-])c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/ml5002486
521 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm990569e
5311068 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm990569e
835 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm990569e
CHEMBL778 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm990569e
DB00633 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm990569e
521 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
5311068 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
835 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
CHEMBL778 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
DB00633 8186 69 None -2 7 Rat 10.8 pKi = 10.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
49781228 23977 1 None 2 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
CHEMBL1256414 23977 1 None 2 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
155540329 179254 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 426 7 0 6 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4482861 179254 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 426 7 0 6 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
78114674 180505 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 380 7 0 7 2.5 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccc(OC)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4536304 180505 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 380 7 0 7 2.5 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccc(OC)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
155513359 176542 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 471 8 0 8 3.9 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3cccc([N+](=O)[O-])c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4438801 176542 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 471 8 0 8 3.9 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3cccc([N+](=O)[O-])c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
49781228 23977 1 None 2 4 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
CHEMBL1256414 23977 1 None 2 4 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
49781228 23977 1 None 2 4 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
CHEMBL1256414 23977 1 None 2 4 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 196 1 1 1 2.4 c1ccc2c(c1)C[C@]1(c3c[nH]cn3)C[C@H]21 10.1021/jm1006269
11271808 67768 0 None 1 2 Human 10.0 pKi = 10 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 490 9 0 7 3.5 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OCCN(C)C)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL176261 67768 0 None 1 2 Human 10.0 pKi = 10 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 490 9 0 7 3.5 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OCCN(C)C)cc4OC[C@H]32)CC1 10.1021/jm049619s
11306100 175286 0 None -3 2 Human 10.0 pKi = 10 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 477 9 0 7 3.5 COCCOc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL435352 175286 0 None -3 2 Human 10.0 pKi = 10 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 477 9 0 7 3.5 COCCOc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
1588 9105 27 None 1 44 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None 1 44 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None 1 44 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None 1 44 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None 1 44 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
52944548 23924 0 None 1 4 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 2 1 1 3.0 CC[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1255723 23924 0 None 1 4 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 2 1 1 3.0 CC[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
52941512 23970 0 None 1 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 2.6 C[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256378 23970 0 None 1 4 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 2.6 C[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
135519400 70668 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 419 5 1 6 3.2 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(O)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL180470 70668 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 419 5 1 6 3.2 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(O)cc4OC[C@H]32)CC1 10.1021/jm049619s
49781222 24023 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 3.0 C[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256609 24023 0 None 2 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 3.0 C[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
46224879 208326 3 None -1 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 208326 3 None -1 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
124 9755 47 None -4 32 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
2032 9755 47 None -4 32 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
4636 9755 47 None -4 32 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
CHEMBL762 9755 47 None -4 32 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
DB00935 9755 47 None -4 32 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
44330168 11091 0 None -1 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4cccs4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL100879 11091 0 None -1 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4cccs4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
11225779 114509 0 None -1 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cc(F)ccc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL319119 114509 0 None -1 2 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cc(F)ccc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44324972 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL419316 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44324972 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL419316 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
44324800 213727 0 None -5 7 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL91157 213727 0 None -5 7 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
44324972 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL419316 170151 0 None -2 4 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
44324800 213727 0 None -5 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL91157 213727 0 None -5 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
78114597 179263 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 356 6 0 6 2.6 CCOP(=O)(OCC)C1N=CC2C(=O)N(C3CCCCC3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4483022 179263 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 356 6 0 6 2.6 CCOP(=O)(OCC)C1N=CC2C(=O)N(C3CCCCC3)C(=O)C21 10.1021/acs.jmedchem.9b02080
49781887 23916 0 None 3 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
CHEMBL1255617 23916 0 None 3 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
9837136 106714 2 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3ccsc32)c[nH]1 10.1021/jm990569e
CHEMBL286269 106714 2 None - 1 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3ccsc32)c[nH]1 10.1021/jm990569e
9837136 106714 2 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3ccsc32)c[nH]1 10.1021/jm000128r
CHEMBL286269 106714 2 None - 1 Rat 9.5 pKi = 9.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3ccsc32)c[nH]1 10.1021/jm000128r
108094 10196 27 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
526 10196 27 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
528 10196 27 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
CHEMBL10332 10196 27 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1021/jm800250z
10531 8202 21 None -5 24 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -5 24 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -5 24 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -5 24 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -5 24 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
10056237 20516 0 None 47 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 817 13 6 6 7.3 O=C(NCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1195197 20516 0 None 47 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 817 13 6 6 7.3 O=C(NCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL554019 20516 0 None 47 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 817 13 6 6 7.3 O=C(NCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
2803 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
516 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
704 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
CHEMBL134 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
DB00575 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
2803 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
516 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
704 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
CHEMBL134 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
DB00575 7742 58 None 1 19 Rat 9.4 pKi = 9.4 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
11259744 67570 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 461 6 0 7 3.4 CC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL176116 67570 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 461 6 0 7 3.4 CC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
52948958 23925 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 238 3 1 1 3.4 CCC[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1255724 23925 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 238 3 1 1 3.4 CCC[C@H]1[C@@H]2c3ccccc3C[C@]12c1c[nH]cn1 10.1021/jm1006269
102 10899 48 None -5 49 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
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 10.1016/s0960-894x(00)00068-8
3659 10899 48 None -5 49 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
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 10.1016/s0960-894x(00)00068-8
8969 10899 48 None -5 49 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
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 10.1016/s0960-894x(00)00068-8
CHEMBL15245 10899 48 None -5 49 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
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 10.1016/s0960-894x(00)00068-8
DB01392 10899 48 None -5 49 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
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 10.1016/s0960-894x(00)00068-8
52943739 23931 0 None 2 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 2.6 C[C@]12C[C@@]1(c1c[nH]cn1)Cc1ccccc12 10.1021/jm1006269
CHEMBL1255771 23931 0 None 2 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 210 1 1 1 2.6 C[C@]12C[C@@]1(c1c[nH]cn1)Cc1ccccc12 10.1021/jm1006269
44387789 67349 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 433 6 0 6 3.5 COc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL176002 67349 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 433 6 0 6 3.5 COc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
44330114 114859 0 None -1 2 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 453 7 0 8 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccco4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL319530 114859 0 None -1 2 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 453 7 0 8 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccco4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44324906 213566 0 None 3 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 419 6 0 6 3.1 COc1ccc2c(c1)OCC1C2=NOC1CN1CCN(C/C=C/c2ccccc2)CC1 10.1016/s0960-894x(03)00525-0
CHEMBL90247 213566 0 None 3 3 Human 9.3 pKi = 9.3 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 419 6 0 6 3.1 COc1ccc2c(c1)OCC1C2=NOC1CN1CCN(C/C=C/c2ccccc2)CC1 10.1016/s0960-894x(03)00525-0
49781223 24024 0 None 2 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 2 1 1 3.3 CC[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256610 24024 0 None 2 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 2 1 1 3.3 CC[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
9815633 106411 3 None 6 6 Rat 9.3 pKi = 9.3 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
CHEMBL284213 106411 3 None 6 6 Rat 9.3 pKi = 9.3 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
9815633 106411 3 None 6 6 Rat 9.3 pKi = 9.3 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm000128r
CHEMBL284213 106411 3 None 6 6 Rat 9.3 pKi = 9.3 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm000128r
49781005 23986 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256503 23986 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
49781887 23916 0 None 3 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
CHEMBL1255617 23916 0 None 3 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
11214030 67318 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 491 8 0 8 3.1 COCC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL175853 67318 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 491 8 0 8 3.1 COCC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
107715 207724 22 None -6 20 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 207724 22 None -6 20 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 207724 22 None -6 20 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
11765813 19750 0 None 60 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 788 11 6 6 6.5 O=C(NCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1189483 19750 0 None 60 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 788 11 6 6 6.5 O=C(NCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL538808 19750 0 None 60 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 788 11 6 6 6.5 O=C(NCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
13938361 192142 0 None 141 2 Bovine 9.1 pKi = 9.1 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@@H]1CCN2CCc3c(oc4ccccc34)[C@@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL48603 192142 0 None 141 2 Bovine 9.1 pKi = 9.1 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@@H]1CCN2CCc3c(oc4ccccc34)[C@@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
1043 8363 14 None -8 29 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None -8 29 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None -8 29 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None -8 29 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None -8 29 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44324800 213727 0 None -5 7 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL91157 213727 0 None -5 7 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44324887 171794 0 None 2 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 419 6 0 6 3.1 COc1ccc2c(c1)C1=NOC(CN3CCN(C/C=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL422597 171794 0 None 2 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 419 6 0 6 3.1 COc1ccc2c(c1)C1=NOC(CN3CCN(C/C=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44325050 214060 0 None -3 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL93171 214060 0 None -3 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44126269 208263 5 None -2 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 208263 5 None -2 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
49781224 23915 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 238 3 1 1 3.7 CCC[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1255616 23915 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 238 3 1 1 3.7 CCC[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
12114852 20092 0 None 31 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 774 10 6 6 6.1 O=C(NCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1192051 20092 0 None 31 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 774 10 6 6 6.1 O=C(NCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL543232 20092 0 None 31 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 774 10 6 6 6.1 O=C(NCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
11785068 67330 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 487 7 0 7 3.8 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)C5CC5)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL175911 67330 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 487 7 0 7 3.8 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)C5CC5)cc4OC[C@H]32)CC1 10.1021/jm049619s
11260018 70633 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 473 7 0 7 3.6 C=CC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL180322 70633 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 473 7 0 7 3.6 C=CC(=O)Oc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
71450907 85714 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 389 5 0 5 3.1 C(=C/c1ccccc1)\CN1CCN(C[C@@H]2ON=C3c4ccccc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL2112978 85714 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 389 5 0 5 3.1 C(=C/c1ccccc1)\CN1CCN(C[C@@H]2ON=C3c4ccccc4OC[C@H]32)CC1 10.1021/jm049619s
44324937 213692 0 None 1 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 389 5 0 5 3.1 C(=C/c1ccccc1)\CN1CCN(CC2ON=C3c4ccccc4OCC32)CC1 10.1016/s0960-894x(03)00525-0
CHEMBL90943 213692 0 None 1 3 Human 9.1 pKi = 9.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 389 5 0 5 3.1 C(=C/c1ccccc1)\CN1CCN(CC2ON=C3c4ccccc4OCC32)CC1 10.1016/s0960-894x(03)00525-0
2142 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
4920903 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
502 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
5775 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
CHEMBL597 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
DB00692 9870 58 None 1 37 Bovine 9.0 pKi = 9.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
155547631 180473 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 432 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C3CCCCC3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4535472 180473 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 432 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C3CCCCC3)C(=O)C21 10.1021/acs.jmedchem.9b02080
11318438 172763 0 None -1 2 Human 9.0 pKi = 9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 524 7 0 8 4.1 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)c5ccncc5)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL425324 172763 0 None -1 2 Human 9.0 pKi = 9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 524 7 0 8 4.1 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)c5ccncc5)cc4OC[C@H]32)CC1 10.1021/jm049619s
9805944 63001 37 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [125I]HEAT from adrenergic alpha2A receptorDisplacement of [125I]HEAT from adrenergic alpha2A receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 63001 37 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [125I]HEAT from adrenergic alpha2A receptorDisplacement of [125I]HEAT from adrenergic alpha2A receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
44330635 215205 0 None -2 2 Human 9.0 pKi = 9 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 493 8 0 8 3.5 COc1ccccc1/C=C(\C)CN1CCN(C[C@@H]2ON=C3c4cc(OC)c(OC)cc4OC[C@H]32)CC1 10.1016/j.bmcl.2004.03.031
CHEMBL99868 215205 0 None -2 2 Human 9.0 pKi = 9 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 493 8 0 8 3.5 COc1ccccc1/C=C(\C)CN1CCN(C[C@@H]2ON=C3c4cc(OC)c(OC)cc4OC[C@H]32)CC1 10.1016/j.bmcl.2004.03.031
52950140 23930 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 1 1 1 3.0 CC1(C)[C@@H]2c3ccccc3C[C@@]21c1c[nH]cn1 10.1021/jm1006269
CHEMBL1255770 23930 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 224 1 1 1 3.0 CC1(C)[C@@H]2c3ccccc3C[C@@]21c1c[nH]cn1 10.1021/jm1006269
44330668 11208 0 None -5 2 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccsc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL101596 11208 0 None -5 2 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccsc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44330617 103395 0 None -5 2 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccc(F)c4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL263424 103395 0 None -5 2 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccc(F)c4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44371848 20397 0 None 15 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 845 15 6 6 8.1 O=C(NCCCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1194334 20397 0 None 15 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 845 15 6 6 8.1 O=C(NCCCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL551711 20397 0 None 15 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 845 15 6 6 8.1 O=C(NCCCCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
9837551 108401 0 None 7 3 Human 8.9 pKi = 8.9 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 232 1 3 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCO2 10.1021/jm960359r
CHEMBL298936 108401 0 None 7 3 Human 8.9 pKi = 8.9 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 232 1 3 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCO2 10.1021/jm960359r
12114853 19800 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 803 12 6 6 6.9 O=C(NCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1189875 19800 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 803 12 6 6 6.9 O=C(NCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL539606 19800 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 803 12 6 6 6.9 O=C(NCCCCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
10847653 64219 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 240 0 1 2 2.6 C1=NC[C@]2(CC[C@@H]3Cc4ccccc4C[C@H]3C2)N1 10.1021/jm001040g
CHEMBL165529 64219 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 240 0 1 2 2.6 C1=NC[C@]2(CC[C@@H]3Cc4ccccc4C[C@H]3C2)N1 10.1021/jm001040g
11785961 70054 0 None -6 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 535 13 0 8 4.0 CCOCCOCCOc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL179237 70054 0 None -6 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 535 13 0 8 4.0 CCOCCOCCOc1ccc2c(c1)OC[C@@H]1C2=NO[C@H]1CN1CCN(C/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
11190988 138581 0 None -2 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 487 7 0 6 4.8 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC5CCCC5)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL369378 138581 0 None -2 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 487 7 0 6 4.8 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC5CCCC5)cc4OC[C@H]32)CC1 10.1021/jm049619s
136019934 151308 0 None -7 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
CHEMBL390718 151308 0 None -7 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
44324737 214017 0 None -2 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL92860 214017 0 None -2 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
44324737 214017 0 None -2 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL92860 214017 0 None -2 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
10123375 20022 0 None 123 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 760 9 6 6 5.8 O=C(NCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1191431 20022 0 None 123 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 760 9 6 6 5.8 O=C(NCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL542527 20022 0 None 123 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 760 9 6 6 5.8 O=C(NCCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
13938356 191857 0 None 154 2 Bovine 8.9 pKi = 8.9 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN(C1CCN2CCc3c(oc4ccccc34)C2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL48558 191857 0 None 154 2 Bovine 8.9 pKi = 8.9 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN(C1CCN2CCc3c(oc4ccccc34)C2C1)S(=O)(=O)CCO 10.1021/jm00150a002
44330369 118359 0 None -4 2 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccsc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL328195 118359 0 None -4 2 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccsc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
102 10899 48 None -5 49 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
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 10.1016/j.bmcl.2005.03.116
3659 10899 48 None -5 49 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
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 10.1016/j.bmcl.2005.03.116
8969 10899 48 None -5 49 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
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 10.1016/j.bmcl.2005.03.116
CHEMBL15245 10899 48 None -5 49 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
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 10.1016/j.bmcl.2005.03.116
DB01392 10899 48 None -5 49 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
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 10.1016/j.bmcl.2005.03.116
44325049 118300 0 None -2 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C(\C)c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL327875 118300 0 None -2 3 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C(\C)c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
10707358 186064 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 272 4 1 3 3.2 c1ccc(CC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL47313 186064 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 272 4 1 3 3.2 c1ccc(CC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
12575 8769 30 None 1 17 Bovine 8.8 pKi = 8.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
54459 8769 30 None 1 17 Bovine 8.8 pKi = 8.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
CHEMBL10316 8769 30 None 1 17 Bovine 8.8 pKi = 8.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm00366a007
9815610 106709 19 None 13 4 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm990569e
CHEMBL286246 106709 19 None 13 4 Rat 8.8 pKi = 8.8 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm990569e
124 9755 47 None -5 32 Bovine 8.8 pKi = 8.8 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
2032 9755 47 None -5 32 Bovine 8.8 pKi = 8.8 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
4636 9755 47 None -5 32 Bovine 8.8 pKi = 8.8 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
CHEMBL762 9755 47 None -5 32 Bovine 8.8 pKi = 8.8 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
DB00935 9755 47 None -5 32 Bovine 8.8 pKi = 8.8 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
9815610 106709 19 None 13 4 Rat 8.8 pKi = 8.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm000128r
CHEMBL286246 106709 19 None 13 4 Rat 8.8 pKi = 8.8 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm000128r
11200476 85706 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for Alpha-2A adrenergic receptorBinding affinity for Alpha-2A adrenergic receptor
ChEMBL 402 5 0 5 3.2 CN1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
CHEMBL2112970 85706 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for Alpha-2A adrenergic receptorBinding affinity for Alpha-2A adrenergic receptor
ChEMBL 402 5 0 5 3.2 CN1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
9837600 30092 0 None 12 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 236 0 1 3 1.9 NC1=NC2(CCc3cccc(Cl)c3C2)CO1 10.1021/jm00020a021
CHEMBL133231 30092 0 None 12 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 236 0 1 3 1.9 NC1=NC2(CCc3cccc(Cl)c3C2)CO1 10.1021/jm00020a021
46891598 13948 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]rauwolscine from adrenergic alpha2A receptorDisplacement of [3H]rauwolscine from adrenergic alpha2A receptor
ChEMBL 402 5 0 5 3.2 CN1CC2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2010.04.099
CHEMBL1085510 13948 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]rauwolscine from adrenergic alpha2A receptorDisplacement of [3H]rauwolscine from adrenergic alpha2A receptor
ChEMBL 402 5 0 5 3.2 CN1CC2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2010.04.099
42266865 22375 2 None 1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 389 6 1 4 3.4 COc1ccccc1N1CCN(CCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221498 22375 2 None 1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 389 6 1 4 3.4 COc1ccccc1N1CCN(CCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
2142 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
4920903 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
502 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
5775 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
CHEMBL597 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
DB00692 9870 58 None -2 37 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/np50094a001
10176999 110331 21 None 11 3 Human 8.8 pKi = 8.8 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
CHEMBL308570 110331 21 None 11 3 Human 8.8 pKi = 8.8 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 231 2 2 4 2.2 Cc1c(Nc2ncc[nH]2)ccc2c1OCCO2 10.1021/jm9605142
44330653 215011 0 None -8 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccs4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL98646 215011 0 None -8 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 469 7 0 8 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccs4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44330645 215213 0 None -3 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 453 7 0 8 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccco4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL99916 215213 0 None -3 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 453 7 0 8 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccco4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
10350094 20589 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 746 8 6 6 5.4 O=C(NCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1195716 20589 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 746 8 6 6 5.4 O=C(NCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL555190 20589 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 746 8 6 6 5.4 O=C(NCCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
49781005 23986 0 None 3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256503 23986 0 None 3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
13123525 195977 0 None - 1 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 265 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)c2ccccc2)cc1 10.1021/jm00366a022
CHEMBL51131 195977 0 None - 1 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 265 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)c2ccccc2)cc1 10.1021/jm00366a022
13123534 196232 1 None - 1 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/jm00366a022
CHEMBL51358 196232 1 None - 1 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/jm00366a022
71461647 85708 0 None 3 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 439 5 0 5 4.4 COc1ccc2c(c1)C=C[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm049619s
CHEMBL2112972 85708 0 None 3 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 439 5 0 5 4.4 COc1ccc2c(c1)C=C[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm049619s
71456240 85717 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 415 6 0 5 3.8 COc1ccc2c(c1)C=C[C@@H]1C2=NO[C@H]1CN1CCN(C/C=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL2112982 85717 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 415 6 0 5 3.8 COc1ccc2c(c1)C=C[C@@H]1C2=NO[C@H]1CN1CCN(C/C=C/c2ccccc2)CC1 10.1021/jm049619s
102 10899 48 None -5 49 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
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 10.1016/j.bmcl.2006.12.094
3659 10899 48 None -5 49 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
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 10.1016/j.bmcl.2006.12.094
8969 10899 48 None -5 49 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
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 10.1016/j.bmcl.2006.12.094
CHEMBL15245 10899 48 None -5 49 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
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 10.1016/j.bmcl.2006.12.094
DB01392 10899 48 None -5 49 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
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 10.1016/j.bmcl.2006.12.094
12576 7302 94 None -2 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm1006269
71310 7302 94 None -2 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm1006269
CHEMBL353972 7302 94 None -2 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm1006269
DB11481 7302 94 None -2 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm1006269
44330368 118969 0 None -3 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 479 7 1 8 3.2 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(O)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL329065 118969 0 None -3 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 479 7 1 8 3.2 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(O)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
108094 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1016/j.ejmech.2014.05.057
526 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1016/j.ejmech.2014.05.057
528 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1016/j.ejmech.2014.05.057
CHEMBL10332 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 10.1016/j.ejmech.2014.05.057
42631003 206397 13 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 206397 13 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
10198135 211904 3 None 43 3 Human 8.0 pKi = 8 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 203 3 2 3 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1 10.1021/jm9605142
CHEMBL77913 211904 3 None 43 3 Human 8.0 pKi = 8 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 203 3 2 3 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1 10.1021/jm9605142
2389 10104 118 None -77 66 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
5073 10104 118 None -77 66 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
96 10104 118 None -77 66 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
CHEMBL85 10104 118 None -77 66 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
DB00734 10104 118 None -77 66 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
44401243 175273 0 None -4 9 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL435301 175273 0 None -4 9 Human 8.0 pKi = 8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
49836302 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276139 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml400232p
10176715 163913 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 2 2.4 C1=NCC(CC2=Cc3ccccc3CC2)N1 10.1021/jm001040g
CHEMBL407509 163913 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 2 2.4 C1=NCC(CC2=Cc3ccccc3CC2)N1 10.1021/jm001040g
242 7258 124 None -26 51 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 7258 124 None -26 51 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 7258 124 None -26 51 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 7258 124 None -26 51 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 7258 124 None -26 51 Human 7.0 pKi = 7 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A 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
250 10159 8 None -2818 13 Human 7.0 pKi = 7 Binding
Compound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
5311416 10159 8 None -2818 13 Human 7.0 pKi = 7 Binding
Compound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
CHEMBL69733 10159 8 None -2818 13 Human 7.0 pKi = 7 Binding
Compound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assayCompound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
135398737 7745 93 None -10 90 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
38 7745 93 None -10 90 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
722 7745 93 None -10 90 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
CHEMBL42 7745 93 None -10 90 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
DB00363 7745 93 None -10 90 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
49836302 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276139 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/jm100977d
49836302 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml300064v
CHEMBL1276139 25338 1 None 1 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@H](C)C1=NCCN1 10.1021/ml300064v
13938357 108507 0 None 79 2 Bovine 7.0 pKi = 7 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@H]1CCN2CCc3c(oc4ccccc34)[C@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
CHEMBL299595 108507 0 None 79 2 Bovine 7.0 pKi = 7 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
ChEMBL 364 4 1 5 1.7 CN([C@H]1CCN2CCc3c(oc4ccccc34)[C@H]2C1)S(=O)(=O)CCO 10.1021/jm00150a002
135398737 7745 93 None -26 90 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 7745 93 None -26 90 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 7745 93 None -26 90 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 7745 93 None -26 90 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 7745 93 None -26 90 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 9688 112 None -93 65 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 9688 112 None -93 65 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 9688 112 None -93 65 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 9688 112 None -93 65 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A 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
2389 10104 118 None -77 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 10104 118 None -77 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 10104 118 None -77 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 10104 118 None -77 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 10104 118 None -77 66 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A 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
90644728 119529 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 1 2.1 CC1CN/C(=N/c2ccc3c(c2)CCCC3)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3289543 119529 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 1 2.1 CC1CN/C(=N/c2ccc3c(c2)CCCC3)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3305161 119529 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 1 2.1 CC1CN/C(=N/c2ccc3c(c2)CCCC3)N1 10.1016/j.ejmech.2014.05.057
16090600 175960 0 None -10 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1021/jm060262x
CHEMBL440594 175960 0 None -10 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 6 2 4 5.1 Cc1nc2ccccc2c(Nc2ccc(NCCN3CCCC3)cc2)c1C 10.1021/jm060262x
10324985 83556 8 None -741 17 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha-2A receptorBinding affinity to adrenergic alpha-2A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 83556 8 None -741 17 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha-2A receptorBinding affinity to adrenergic alpha-2A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 83556 8 None -741 17 Human 6.0 pKi = 6 Binding
Binding affinity to adrenergic alpha-2A receptorBinding affinity to adrenergic alpha-2A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
127035062 143229 0 None -3 19 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha 2A receptor stably expressed in MDCK cells after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human recombinant alpha 2A receptor stably expressed in MDCK cells after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 143229 0 None -3 19 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha 2A receptor stably expressed in MDCK cells after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human recombinant alpha 2A receptor stably expressed in MDCK cells after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
10443343 25272 1 None - 1 Bovine 6.0 pKi = 6.0 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 0 5 0.5 CN1CCN(c2nccn3ccnc23)CC1 10.1021/jm00099a012
CHEMBL127303 25272 1 None - 1 Bovine 6.0 pKi = 6.0 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 0 5 0.5 CN1CCN(c2nccn3ccnc23)CC1 10.1021/jm00099a012
1782 9296 84 None -5 23 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 9296 84 None -5 23 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 9296 84 None -5 23 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 9296 84 None -5 23 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 9296 84 None -5 23 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
44574076 179240 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448147 179240 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
9960497 123853 0 None -309 6 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL3392246 123853 0 None -309 6 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
57395731 77965 0 None 6 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 232 4 1 4 1.7 CC(=O)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956202 77965 0 None 6 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 232 4 1 4 1.7 CC(=O)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
44312037 211398 1 None 1 6 Human 5.0 pKi = 5.0 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73392 211398 1 None 1 6 Human 5.0 pKi = 5.0 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 308 1 1 5 2.9 Brc1c(NC2=NCCS2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
3151 8244 97 None -99 26 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 8244 97 None -99 26 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 8244 97 None -99 26 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 8244 97 None -99 26 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 8244 97 None -99 26 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
12909387 69411 0 None -33 2 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 301 0 0 3 3.8 CN1CCC(=C2c3cc(C#N)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL178376 69411 0 None -33 2 Bovine 6.0 pKi = 6.0 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 301 0 0 3 3.8 CN1CCC(=C2c3cc(C#N)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
9904117 16174 3 None 1 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111554 16174 3 None 1 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
11091738 124870 0 None -3 5 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
CHEMBL340641 124870 0 None -3 5 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
57402718 77964 2 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956201 77964 2 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 4 1 4 1.3 CC(Oc1ccccc1C=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
2803 7742 58 None -1 19 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 7742 58 None -1 19 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 7742 58 None -1 19 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 7742 58 None -1 19 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 7742 58 None -1 19 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
16090624 89176 0 None -13 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
CHEMBL217278 89176 0 None -13 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
4209 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 9937 75 None -74 33 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
277 8083 62 None -33 50 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 8083 62 None -33 50 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 8083 62 None -33 50 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 8083 62 None -33 50 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 8083 62 None -33 50 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
1268096 22937 26 None -3 4 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]12 10.1021/jm00019a001
CHEMBL122404 22937 26 None -3 4 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]12 10.1021/jm00019a001
90644708 119519 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 5 3 3 2.4 CCNc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289530 119519 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 5 3 3 2.4 CCNc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304993 119519 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 5 3 3 2.4 CCNc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
68617 212306 62 None -3 26 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 212306 62 None -3 26 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 212306 62 None -3 26 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
10769331 118310 0 None -208 6 Human 7.0 pKi = 7.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 566 9 2 7 5.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1021/jm980077m
CHEMBL327931 118310 0 None -208 6 Human 7.0 pKi = 7.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 566 9 2 7 5.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc(Cl)c([N+](=O)[O-])c1 10.1021/jm980077m
197033 205931 64 None -13 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 205931 64 None -13 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cellsDisplacement of [3H]MK-912 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
13298529 107996 57 None 134 2 Bovine 8.0 pKi = 8.0 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 241 1 1 3 1.3 Brc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL295921 107996 57 None 134 2 Bovine 8.0 pKi = 8.0 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 241 1 1 3 1.3 Brc1cccnc1N1CCNCC1 10.1021/jm00366a007
71456238 85713 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 504 9 0 7 4.4 COc1cc2c(cc1OC)N(C)C[C@@H]1C2=NO[C@H]1CN1CCN(CCC/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
CHEMBL2112977 85713 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 504 9 0 7 4.4 COc1cc2c(cc1OC)N(C)C[C@@H]1C2=NO[C@H]1CN1CCN(CCC/C(C)=C/c2ccccc2)CC1 10.1021/jm049619s
46934426 22397 0 None 4 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 431 9 1 4 4.6 COc1ccccc1N1CCN(CCCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221591 22397 0 None 4 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 431 9 1 4 4.6 COc1ccccc1N1CCN(CCCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
49781004 23985 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@@H]1c2ccccc2[C@H]2C[C@]21c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256502 23985 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@@H]1c2ccccc2[C@H]2C[C@]21c1c[nH]cn1 10.1021/jm1006269
44371755 55551 0 None 15 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 3 1 3 2.1 Cc1cccc(C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL155866 55551 0 None 15 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 3 1 3 2.1 Cc1cccc(C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
90469115 192621 4 None -36 17 Human 7.0 pKi = 7.0 Binding
Binding affinity to human adrenergic alpha 2A receptorBinding affinity to human adrenergic alpha 2A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 192621 4 None -36 17 Human 7.0 pKi = 7.0 Binding
Binding affinity to human adrenergic alpha 2A receptorBinding affinity to human adrenergic alpha 2A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
9809007 179343 8 None -1905 6 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL448620 179343 8 None -1905 6 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
10109188 172854 0 None -43 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
CHEMBL425803 172854 0 None -43 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 4 1 4 4.6 CCc1c(C)nc2ccccc2c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
44574103 179367 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448908 179367 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
162661022 188227 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 485 9 5 11 0.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4764318 188227 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 485 9 5 11 0.5 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
3168 16034 92 None -123 22 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 16034 92 None -123 22 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
1227 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 9267 43 None -91 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2435 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 7509 100 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
44574079 196088 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL512289 196088 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
10531766 213776 0 None -999 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 607 9 2 7 6.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL91415 213776 0 None -999 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 607 9 2 7 6.3 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
62381476 119544 2 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 4 3 2 2.1 CCCNC(=N)Nc1ccc(N(C)C)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289536 119544 2 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 4 3 2 2.1 CCCNC(=N)Nc1ccc(N(C)C)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305461 119544 2 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 4 3 2 2.1 CCCNC(=N)Nc1ccc(N(C)C)cc1 10.1016/j.ejmech.2014.05.057
122295 16640 7 None -1 9 Human 6.9 pKi = 6.9 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
CHEMBL114166 16640 7 None -1 9 Human 6.9 pKi = 6.9 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
122295 16640 7 None -1 9 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
CHEMBL114166 16640 7 None -1 9 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00019a001
44574104 196268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513871 196268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
145990586 173622 0 None -89 11 Human 5.9 pKi = 5.9 Binding
Binding affinity to andrenergic alpha2A receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic alpha2A receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 173622 0 None -89 11 Human 5.9 pKi = 5.9 Binding
Binding affinity to andrenergic alpha2A receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic alpha2A receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
2335 18620 22 None -5 12 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 18620 22 None -5 12 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 18620 22 None -5 12 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 18620 22 None -5 12 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
176 7186 66 None -3 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -3 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -3 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -3 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -3 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44424855 92229 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
CHEMBL226636 92229 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
44325038 213695 0 None -3 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 474 6 0 8 3.2 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccc5ncccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL90966 213695 0 None -3 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 474 6 0 8 3.2 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccc5ncccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
127026052 144331 0 None -7 19 Human 6.9 pKi = 6.9 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 144331 0 None -7 19 Human 6.9 pKi = 6.9 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
16090630 90012 0 None -309 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 4 2 5 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)(C)C3)cc2)c1CO 10.1021/jm060262x
CHEMBL218675 90012 0 None -309 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 4 2 5 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)(C)C3)cc2)c1CO 10.1021/jm060262x
10579368 112781 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL313251 112781 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 9 3 6 5.3 CC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
155526524 177964 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 364 6 0 6 2.4 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4459090 177964 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 364 6 0 6 2.4 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C)C(=O)C21 10.1021/acs.jmedchem.9b02080
90644720 119535 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 3 4 4 0.3 N=C(NCCO)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3289524 119535 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 3 4 4 0.3 N=C(NCCO)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3305319 119535 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 3 4 4 0.3 N=C(NCCO)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
44579230 188323 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 468 10 1 7 2.8 CCCCOc1cccc(C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)n1 10.1016/j.bmcl.2008.08.055
CHEMBL476569 188323 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 468 10 1 7 2.8 CCCCOc1cccc(C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)n1 10.1016/j.bmcl.2008.08.055
10316512 23639 2 None -18 2 Bovine 4.9 pKi = 4.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 359 1 1 5 1.7 Brc1cnc(N2CCNCC2)c2ncc(Br)n12 10.1021/jm00099a012
CHEMBL124926 23639 2 None -18 2 Bovine 4.9 pKi = 4.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 359 1 1 5 1.7 Brc1cnc(N2CCNCC2)c2ncc(Br)n12 10.1021/jm00099a012
10081626 27867 0 None 12 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 204 0 1 2 1.7 Fc1cccc2c1CC1(CC2)CN=CN1 10.1021/jm00020a021
CHEMBL131220 27867 0 None 12 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 204 0 1 2 1.7 Fc1cccc2c1CC1(CC2)CN=CN1 10.1021/jm00020a021
10262765 123333 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1cccc2c1CCC1(CN=CN1)C2 10.1021/jm00020a021
CHEMBL336332 123333 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1cccc2c1CCC1(CN=CN1)C2 10.1021/jm00020a021
398712 84644 5 None -12 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cellsDisplacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cells
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
CHEMBL209324 84644 5 None -12 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cellsDisplacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cells
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
44325075 118542 0 None -2 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 465 8 0 8 2.7 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCC(=O)c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL328735 118542 0 None -2 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 465 8 0 8 2.7 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCC(=O)c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44292196 186785 2 None 5 2 Bovine 6.9 pKi = 6.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 287 3 0 3 3.1 Clc1cccnc1N1CCN(Cc2ccccc2)CC1 10.1021/jm00366a007
CHEMBL47471 186785 2 None 5 2 Bovine 6.9 pKi = 6.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 287 3 0 3 3.1 Clc1cccnc1N1CCN(Cc2ccccc2)CC1 10.1021/jm00366a007
9809007 179343 8 None -1905 6 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL448620 179343 8 None -1905 6 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
2775690 99786 53 None -45 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2A adrenoceptor receptor (unknown origin)Binding affinity to alpha2A adrenoceptor receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 99786 53 None -45 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2A adrenoceptor receptor (unknown origin)Binding affinity to alpha2A adrenoceptor receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
9809007 179343 8 None -1905 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL448620 179343 8 None -1905 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
11380132 91194 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccccn1)C1=NCCN1 10.1021/jm0408215
CHEMBL221989 91194 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccccn1)C1=NCCN1 10.1021/jm0408215
1268096 22937 26 None -42 4 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for the ability to inhibit binding of [3H]nitrendipine to membrane homogenates of of rat alpha-2D adrenergic receptorCompound was evaluated for the ability to inhibit binding of [3H]nitrendipine to membrane homogenates of of rat alpha-2D adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]12 10.1021/jm00019a001
CHEMBL122404 22937 26 None -42 4 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for the ability to inhibit binding of [3H]nitrendipine to membrane homogenates of of rat alpha-2D adrenergic receptorCompound was evaluated for the ability to inhibit binding of [3H]nitrendipine to membrane homogenates of of rat alpha-2D adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@H]3C[C@H]12 10.1021/jm00019a001
92766 113319 35 None -12 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
CHEMBL31410 113319 35 None -12 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
24839550 144093 14 None -1 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 144093 14 None -1 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
11246610 91087 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccc([N+](=O)[O-])cc1)C1=NCCN1 10.1021/jm0408215
CHEMBL221523 91087 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccc([N+](=O)[O-])cc1)C1=NCCN1 10.1021/jm0408215
16090626 88910 0 None -77 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 378 3 1 4 4.9 Cc1nc2ccc(F)cc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL216727 88910 0 None -77 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 378 3 1 4 4.9 Cc1nc2ccc(F)cc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
44421258 91521 0 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL1204386 91521 0 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL222933 91521 0 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
90644730 119548 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 3 3 2 1.7 CCNc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289544 119548 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 3 3 2 1.7 CCNc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305465 119548 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 3 3 2 1.7 CCNc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
71452341 90472 7 None -4 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
CHEMBL2205361 90472 7 None -4 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
44269006 39127 1 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL14107 39127 1 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 5 1 3 1.8 C=CCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
24906243 194027 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2cccc(-c3ccccc3)c2O1 10.1021/jm800250z
CHEMBL492648 194027 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2cccc(-c3ccccc3)c2O1 10.1021/jm800250z
1267 10576 49 None -52 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
3035905 10576 49 None -52 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
CHEMBL260374 10576 49 None -52 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
2284 9956 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 9956 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 9956 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 9956 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 9956 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
9839050 119156 0 None -263 9 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
CHEMBL329566 119156 0 None -263 9 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
9928335 126875 2 None -3 6 Rat 6.9 pKi = 6.9 Binding
In vivo binding affinity was evaluated against Alpha-1 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-1 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35093 126875 2 None -3 6 Rat 6.9 pKi = 6.9 Binding
In vivo binding affinity was evaluated against Alpha-1 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-1 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL4520788 220754 10 None -6 25 Human 6.9 pKi = 6.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA2ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA2A
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
3038525 20321 114 None -2 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 435 3 0 5 5.5 O=c1ncn2nc(Sc3ccc(F)cc3F)ccc2c1-c1c(Cl)cccc1Cl nan
CHEMBL119385 20321 114 None -2 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 435 3 0 5 5.5 O=c1ncn2nc(Sc3ccc(F)cc3F)ccc2c1-c1c(Cl)cccc1Cl nan
181743 185351 5 None -645 22 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Clonidine from human adrenergic alpha2A receptorDisplacement of [3H]Clonidine from human adrenergic alpha2A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 185351 5 None -645 22 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Clonidine from human adrenergic alpha2A receptorDisplacement of [3H]Clonidine from human adrenergic alpha2A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
9827677 175201 0 None -6456 7 Human 5.9 pKi = 5.9 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43491 175201 0 None -6456 7 Human 5.9 pKi = 5.9 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
10627021 113872 0 None -933 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 577 9 2 5 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm980077m
CHEMBL315914 113872 0 None -933 6 Human 5.9 pKi = 5.9 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 577 9 2 5 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C)cc1 10.1021/jm980077m
129211 10521 78 None -120 16 Human 7.9 pKi = 7.9 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 10521 78 None -120 16 Human 7.9 pKi = 7.9 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 10521 78 None -120 16 Human 7.9 pKi = 7.9 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 10521 78 None -120 16 Human 7.9 pKi = 7.9 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 10521 78 None -120 16 Human 7.9 pKi = 7.9 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
44292385 107898 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL295186 107898 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 270 3 1 3 2.6 c1ccc(C[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
10609673 110553 0 None 11 3 Human 6.9 pKi = 6.9 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 233 4 2 4 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1OC 10.1021/jm9605142
CHEMBL308863 110553 0 None 11 3 Human 6.9 pKi = 6.9 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 233 4 2 4 2.5 COc1ccc(Nc2ncc[nH]2)c(C)c1OC 10.1021/jm9605142
CHEMBL179334 70077 0 None -7079 6 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)[C@H]1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
162664874 188955 0 None - 1 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 519 9 5 11 1.1 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccc(Cl)cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4782649 188955 0 None - 1 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 519 9 5 11 1.1 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccc(Cl)cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
71450550 90582 0 None -2 16 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2A adrenergic receptorBinding affinity to alpha2A adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 90582 0 None -2 16 Human 5.9 pKi = 5.9 Binding
Binding affinity to alpha2A adrenergic receptorBinding affinity to alpha2A adrenergic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
9926529 16161 2 None -1 5 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111496 16161 2 None -1 5 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
10221004 211010 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 211010 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
90644736 119549 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 3 2 3 2.3 CN(C)c1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289547 119549 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 3 2 3 2.3 CN(C)c1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305466 119549 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 3 2 3 2.3 CN(C)c1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
180 7189 56 None -58 40 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 7189 56 None -58 40 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 7189 56 None -58 40 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 7189 56 None -58 40 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 7189 56 None -58 40 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2726 7706 68 None -87 72 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -87 72 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -87 72 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -87 72 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -87 72 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
10475736 172642 0 None -26 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 4 2 5 4.1 CN1CCN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CC1(C)C 10.1021/jm060262x
CHEMBL424917 172642 0 None -26 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 4 2 5 4.1 CN1CCN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CC1(C)C 10.1021/jm060262x
3805301 108114 83 None -1 2 Bovine 5.9 pKi = 5.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
CHEMBL296787 108114 83 None -1 2 Bovine 5.9 pKi = 5.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
CHEMBL1350036 74572 0 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1909062 74572 0 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
44438148 100265 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL246229 100265 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 10.1016/j.bmcl.2006.12.094
11779308 25275 8 None 4 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 295 1 0 5 1.2 CN1CCN(c2nccn3c(Br)cnc23)CC1 10.1021/jm00099a012
CHEMBL127318 25275 8 None 4 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 295 1 0 5 1.2 CN1CCN(c2nccn3c(Br)cnc23)CC1 10.1021/jm00099a012
44288877 175378 0 None -1905 5 Human 4.9 pKi = 4.9 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL43594 175378 0 None -1905 5 Human 4.9 pKi = 4.9 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
2484 215072 71 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 nan
CHEMBL990 215072 71 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 nan
599482 209763 9 None -9 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards alpha-2A-Adrenergic receptorBinding affinity towards alpha-2A-Adrenergic receptor
ChEMBL 202 1 2 2 1.8 COc1ccc2c3c([nH]c2c1)CNCC3 10.1016/j.bmcl.2003.09.027
CHEMBL6310 209763 9 None -9 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards alpha-2A-Adrenergic receptorBinding affinity towards alpha-2A-Adrenergic receptor
ChEMBL 202 1 2 2 1.8 COc1ccc2c3c([nH]c2c1)CNCC3 10.1016/j.bmcl.2003.09.027
119584 9373 102 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 9373 102 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 9373 102 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 9373 102 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 9373 102 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
44579228 188433 0 None -57 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 467 7 2 7 2.9 CC(C)(C)Nc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL477608 188433 0 None -57 3 Human 6.9 pKi = 6.9 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 467 7 2 7 2.9 CC(C)(C)Nc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
11265631 143187 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
CHEMBL373535 143187 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm061487a
11265631 143187 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
CHEMBL373535 143187 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1cccnc1)C1=NCCN1 10.1021/jm0408215
10317643 105316 0 None -32 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
CHEMBL276417 105316 0 None -32 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 380 4 2 5 3.8 CC1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
2737203 190703 83 None 141 2 Bovine 7.9 pKi = 7.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 188 1 1 4 0.4 N#Cc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL48137 190703 83 None 141 2 Bovine 7.9 pKi = 7.9 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 188 1 1 4 0.4 N#Cc1cccnc1N1CCNCC1 10.1021/jm00366a007
13123527 108567 3 None - 1 Bovine 7.9 pKi = 7.9 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 189 3 2 3 1.4 Cc1ccc(NCC2=NCCN2)cc1 10.1021/jm00366a022
CHEMBL300053 108567 3 None - 1 Bovine 7.9 pKi = 7.9 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 189 3 2 3 1.4 Cc1ccc(NCC2=NCCN2)cc1 10.1021/jm00366a022
13123531 195020 0 None - 1 Bovine 7.9 pKi = 7.9 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 217 4 1 3 1.8 CCN(CC1=NCCN1)c1ccc(C)cc1 10.1021/jm00366a022
CHEMBL49953 195020 0 None - 1 Bovine 7.9 pKi = 7.9 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 217 4 1 3 1.8 CCN(CC1=NCCN1)c1ccc(C)cc1 10.1021/jm00366a022
10219 195575 37 None -1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL493439 195575 37 None -1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL50588 195575 37 None -1 5 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
11211035 91778 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL223836 91778 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm061487a
11211035 91778 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL223836 91778 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 284 4 1 3 3.3 CC(Oc1ccccc1-c1cccc(F)c1)C1=NCCN1 10.1021/jm0408215
10376053 19907 0 None 2 3 Bovine 6.9 pKi = 6.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL1190547 19907 0 None 2 3 Bovine 6.9 pKi = 6.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL541088 19907 0 None 2 3 Bovine 6.9 pKi = 6.9 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
16090622 89073 0 None -165 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1021/jm060262x
CHEMBL217202 89073 0 None -165 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 346 3 1 4 4.4 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)C2)cc1 10.1021/jm060262x
10070896 89971 0 None -281 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 422 4 1 4 6.1 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1-c1ccccc1 10.1021/jm060262x
CHEMBL218457 89971 0 None -281 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 422 4 1 4 6.1 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1-c1ccccc1 10.1021/jm060262x
44438166 100592 0 None -33 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 467 8 2 7 3.5 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCC(C)(C)N)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL247664 100592 0 None -33 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 467 8 2 7 3.5 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCC(C)(C)N)cc13)CC2 10.1016/j.bmcl.2006.12.094
4428003 119541 17 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 179 3 3 2 1.4 CCOc1ccc(NC(=N)N)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289540 119541 17 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 179 3 3 2 1.4 CCOc1ccc(NC(=N)N)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305332 119541 17 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 179 3 3 2 1.4 CCOc1ccc(NC(=N)N)cc1 10.1016/j.ejmech.2014.05.057
155566429 182706 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 378 7 0 6 2.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CC)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4587519 182706 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 378 7 0 6 2.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CC)C(=O)C21 10.1021/acs.jmedchem.9b02080
90644758 119528 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 3 2 2 1.7 CCOc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289541 119528 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 3 2 2 1.7 CCOc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305160 119528 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 3 2 2 1.7 CCOc1ccc(/N=C2/NCC(C)N2)cc1 10.1016/j.ejmech.2014.05.057
5472 212597 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL1717 212597 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
CHEMBL833 212597 75 None -1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 nan
10318507 65727 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 3 1 4 5.4 Cc1nc2cc(Cl)ccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL1689423 65727 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 3 1 4 5.4 Cc1nc2cc(Cl)ccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
2406 107180 89 None -16 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 107180 89 None -16 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
43260 12254 65 None 1 5 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm030551a
CHEMBL1076 12254 65 None 1 5 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1 10.1021/jm030551a
10758200 70191 0 None -43 5 Human 6.8 pKi = 6.8 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 322 4 0 3 3.2 c1ccc(CN2CCN(CC3CCc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL179648 70191 0 None -43 5 Human 6.8 pKi = 6.8 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 322 4 0 3 3.2 c1ccc(CN2CCN(CC3CCc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
1836 9370 59 None -43 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 9370 59 None -43 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 9370 59 None -43 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 9370 59 None -43 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 9370 59 None -43 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
44574135 195957 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL511211 195957 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
90644702 119493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 5 2 3 2.4 CCOc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289533 119493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 5 2 3 2.4 CCOc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304532 119493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 5 2 3 2.4 CCOc1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
44311789 211514 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 345 1 2 5 3.1 Brc1c(NC2=N[C@@H]3CCCC[C@@H]3N2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL74342 211514 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 345 1 2 5 3.1 Brc1c(NC2=N[C@@H]3CCCC[C@@H]3N2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
9894818 105701 0 None -83 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm00019a001
CHEMBL279436 105701 0 None -83 7 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm00019a001
4189 213701 96 None -18 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -18 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -18 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
131268 119679 27 None 26 3 Bovine 7.8 pKi = 7.8 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL331036 119679 27 None 26 3 Bovine 7.8 pKi = 7.8 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
3952 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 8669 38 None -3 12 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
10266032 195660 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL50720 195660 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 286 5 1 3 3.5 c1ccc(CCC[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
12114851 19813 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 732 7 6 6 5.0 O=C(NCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1189965 19813 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 732 7 6 6 5.0 O=C(NCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL539824 19813 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 732 7 6 6 5.0 O=C(NCCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
44292386 108259 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297827 108259 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 296 4 1 3 3.5 C(=C/c1ccccc1)\C[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
13123529 108640 0 None - 1 Bovine 6.8 pKi = 6.8 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 203 3 1 3 1.4 Cc1ccc(N(C)CC2=NCCN2)cc1 10.1021/jm00366a022
CHEMBL300628 108640 0 None - 1 Bovine 6.8 pKi = 6.8 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 203 3 1 3 1.4 Cc1ccc(N(C)CC2=NCCN2)cc1 10.1021/jm00366a022
12574 9383 88 None -33 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
4810 9383 88 None -33 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
CHEMBL19236 9383 88 None -33 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
DB09242 9383 88 None -33 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1021/jm960012o
3584 10549 64 None -251 14 Human 5.8 pKi = 5.8 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
5401 10549 64 None -251 14 Human 5.8 pKi = 5.8 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
7302 10549 64 None -251 14 Human 5.8 pKi = 5.8 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
CHEMBL611 10549 64 None -251 14 Human 5.8 pKi = 5.8 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
DB01162 10549 64 None -251 14 Human 5.8 pKi = 5.8 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm970364a
11041026 187004 48 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 162 1 2 2 0.7 NCC1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c01475
CHEMBL4749860 187004 48 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 162 1 2 2 0.7 NCC1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c01475
162645059 186193 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 471 8 5 11 0.1 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4740168 186193 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 471 8 5 11 0.1 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
162653032 187170 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 505 8 5 11 0.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccc(Cl)cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4751862 187170 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 505 8 5 11 0.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccc(Cl)cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
162654934 187370 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 485 9 5 11 0.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2CNCc3ccccc32)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4754362 187370 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 485 9 5 11 0.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2CNCc3ccccc32)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
9894818 105701 0 None -83 7 Human 6.8 pKi = 6.8 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 105701 0 None -83 7 Human 6.8 pKi = 6.8 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
10474335 201471 23 None -52 10 Human 5.8 pKi = 5.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 201471 23 None -52 10 Human 5.8 pKi = 5.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
90644710 119506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 3 3 4 2.1 N=C(NCc1ccco1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3289529 119506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 3 3 4 2.1 N=C(NCc1ccco1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3304670 119506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 259 3 3 4 2.1 N=C(NCc1ccco1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
44421258 91521 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL1204386 91521 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL222933 91521 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 264 3 1 3 2.8 c1ccc(-c2ccccc2C2OC2C2=NCCN2)cc1 10.1021/jm0408215
62379598 119546 3 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 3 3 3 1.8 CCCNC(=N)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3289539 119546 3 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 3 3 3 1.8 CCCNC(=N)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3305463 119546 3 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 3 3 3 1.8 CCCNC(=N)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
5318 22348 49 None -1 13 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 22348 49 None -1 13 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 22348 49 None -1 13 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
5353853 24758 47 None -16 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 24758 47 None -16 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 24758 47 None -16 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
101333429 123854 0 None -3890 6 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1021/jm00019a001
CHEMBL3392247 123854 0 None -3890 6 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1021/jm00019a001
11186523 134289 0 None -109 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL366164 134289 0 None -109 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
135356876 180853 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human alpha2A receptor expressed in MDCK cells by PDSP assayBinding affinity to human alpha2A receptor expressed in MDCK cells by PDSP assay
ChEMBL 464 5 2 6 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4544251 180853 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human alpha2A receptor expressed in MDCK cells by PDSP assayBinding affinity to human alpha2A receptor expressed in MDCK cells by PDSP assay
ChEMBL 464 5 2 6 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
114697 10459 4 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 263 1 2 3 2.7 Clc1ccc(cc1NC1=NCCN1)C(F)(F)F 10.1021/jm00020a021
513 10459 4 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 263 1 2 3 2.7 Clc1ccc(cc1NC1=NCCN1)C(F)(F)F 10.1021/jm00020a021
CHEMBL101340 10459 4 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 263 1 2 3 2.7 Clc1ccc(cc1NC1=NCCN1)C(F)(F)F 10.1021/jm00020a021
12981869 175415 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 230 2 1 2 2.5 Fc1ccc2c(c1)C=C(CC1CN=CN1)CC2 10.1021/jm001040g
CHEMBL436234 175415 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 230 2 1 2 2.5 Fc1ccc2c(c1)C=C(CC1CN=CN1)CC2 10.1021/jm001040g
10508016 213935 0 None -43 6 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 613 9 2 5 7.7 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1021/jm980077m
CHEMBL92322 213935 0 None -43 6 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 613 9 2 5 7.7 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2ccccc2c1 10.1021/jm980077m
132584404 150127 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Rauwolscine from human Alpha2A receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]Rauwolscine from human Alpha2A receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 416 3 0 2 6.7 CCCN1CC[C@H]2c3cc4ccc(C(F)(F)F)cc4nc3[C@H](CC)[C@H]3CCC[C@@H]1[C@@H]32 10.1016/j.bmcl.2016.10.065
CHEMBL3897499 150127 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Rauwolscine from human Alpha2A receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]Rauwolscine from human Alpha2A receptor expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 416 3 0 2 6.7 CCCN1CC[C@H]2c3cc4ccc(C(F)(F)F)cc4nc3[C@H](CC)[C@H]3CCC[C@@H]1[C@@H]32 10.1016/j.bmcl.2016.10.065
135 9310 43 None -4 56 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 9310 43 None -4 56 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 9310 43 None -4 56 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 9310 43 None -4 56 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 9310 43 None -4 56 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
44324800 213727 0 None -5 7 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL91157 213727 0 None -5 7 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
14004040 58409 0 None 6 2 Bovine 7.8 pKi = 7.8 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL158371 58409 0 None 6 2 Bovine 7.8 pKi = 7.8 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
124 9755 47 None -4 32 Human 7.8 pKi = 7.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 9755 47 None -4 32 Human 7.8 pKi = 7.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 9755 47 None -4 32 Human 7.8 pKi = 7.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 9755 47 None -4 32 Human 7.8 pKi = 7.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 9755 47 None -4 32 Human 7.8 pKi = 7.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
14004040 58409 0 None 6 2 Bovine 7.8 pKi = 7.8 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL158371 58409 0 None 6 2 Bovine 7.8 pKi = 7.8 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 227 0 0 2 3.5 c1ccc2c3c(oc2c1)C1CCCCN1CC3 10.1021/jm00398a025
15391752 189109 0 None -7 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4784373 189109 0 None -7 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
44371744 57095 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 270 7 1 3 2.9 C=CCc1cccc(CC=C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL157206 57095 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 270 7 1 3 2.9 C=CCc1cccc(CC=C)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
11360447 91776 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
CHEMBL223829 91776 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1cccs1)C1=NCCN1 10.1021/jm0408215
44350012 24796 0 None 6 3 Bovine 5.8 pKi = 5.8 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 363 4 3 7 0.4 CC1CN=C2C(N3CCNCC3)=NC=CN21.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
CHEMBL126394 24796 0 None 6 3 Bovine 5.8 pKi = 5.8 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 363 4 3 7 0.4 CC1CN=C2C(N3CCNCC3)=NC=CN21.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
6604117 194626 6 None -16 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL2062340 194626 6 None -16 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL49623 194626 6 None -16 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
168290009 198597 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 267 1 2 5 2.0 Nc1ncc(/C=C2\CCc3c(O)cccc3C2=O)cn1 10.1016/j.ejmech.2021.113964
CHEMBL5198566 198597 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 267 1 2 5 2.0 Nc1ncc(/C=C2\CCc3c(O)cccc3C2=O)cn1 10.1016/j.ejmech.2021.113964
10660 21188 58 None -43 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 21188 58 None -43 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
6918276 22383 7 None -16 8 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 22383 7 None -16 8 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
3198 212292 76 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
11140345 210950 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 210950 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
122442272 145126 0 None -11 15 Human 6.8 pKi = 6.8 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 145126 0 None -11 15 Human 6.8 pKi = 6.8 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 145126 0 None -11 15 Human 6.8 pKi = 6.8 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
49836306 25347 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276247 25347 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
21392988 211596 4 None -1 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 156 0 0 4 -0.3 C1COC(N2CCOCC2)=N1 10.1016/0960-894X(94)85032-1
CHEMBL75201 211596 4 None -1 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 156 0 0 4 -0.3 C1COC(N2CCOCC2)=N1 10.1016/0960-894X(94)85032-1
4209 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 9937 75 None -263 33 Rat 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
1547484 7727 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 7727 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 7727 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 7727 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 7727 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
3645619 9808 20 None -104 9 Rat 6.8 pKi = 6.8 Binding
Binding affinity at alpha-1 adrenergic receptorBinding affinity at alpha-1 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 9808 20 None -104 9 Rat 6.8 pKi = 6.8 Binding
Binding affinity at alpha-1 adrenergic receptorBinding affinity at alpha-1 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 9808 20 None -104 9 Rat 6.8 pKi = 6.8 Binding
Binding affinity at alpha-1 adrenergic receptorBinding affinity at alpha-1 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
132060720 169268 0 None -4 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 169268 0 None -4 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
44415569 172713 0 None -107 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 172713 0 None -107 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
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
26987 7736 33 None -158 21 Human 6.8 pKi = 6.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
6063 7736 33 None -158 21 Human 6.8 pKi = 6.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
671 7736 33 None -158 21 Human 6.8 pKi = 6.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
CHEMBL1626 7736 33 None -158 21 Human 6.8 pKi = 6.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
DB00283 7736 33 None -158 21 Human 6.8 pKi = 6.8 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
9838192 118089 18 None 2 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to Homo sapiens (human) alpha2A receptorBinding affinity to Homo sapiens (human) alpha2A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
CHEMBL326702 118089 18 None 2 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to Homo sapiens (human) alpha2A receptorBinding affinity to Homo sapiens (human) alpha2A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1007/s00044-004-0020-z
155523897 177649 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 444 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccc(F)cc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4454147 177649 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 444 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccc(F)cc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
155556443 181263 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 406 6 0 6 3.6 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C(C)(C)C)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4554450 181263 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 406 6 0 6 3.6 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(C(C)(C)C)C(=O)C21 10.1021/acs.jmedchem.9b02080
9838192 118089 18 None 2 6 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm030551a
CHEMBL326702 118089 18 None 2 6 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1021/jm030551a
136680384 214434 0 None -380 6 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
44328799 214434 0 None -380 6 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
CHEMBL95290 214434 0 None -380 6 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 694 16 4 8 4.9 CCNC(=O)C1=C(CC)NC(COCCN)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
90644742 119517 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 2 2 4 1.9 c1coc(C2CN/C(=N/c3ccc4c(c3)OCO4)N2)c1 10.1016/j.ejmech.2014.05.057
CHEMBL3289550 119517 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 2 2 4 1.9 c1coc(C2CN/C(=N/c3ccc4c(c3)OCO4)N2)c1 10.1016/j.ejmech.2014.05.057
CHEMBL3304990 119517 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 2 2 4 1.9 c1coc(C2CN/C(=N/c3ccc4c(c3)OCO4)N2)c1 10.1016/j.ejmech.2014.05.057
135 9310 43 None -5 56 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
1796 9310 43 None -5 56 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
4184 9310 43 None -5 56 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
CHEMBL6437 9310 43 None -5 56 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
DB06148 9310 43 None -5 56 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00366a007
3303 9024 46 None -251 15 Human 6.8 pKi = 6.8 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 9024 46 None -251 15 Human 6.8 pKi = 6.8 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 9024 46 None -251 15 Human 6.8 pKi = 6.8 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
10319299 88362 0 None -48 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1021/jm060262x
CHEMBL216290 88362 0 None -48 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 408 4 1 4 5.7 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1-c1ccccc1 10.1021/jm060262x
10177445 172821 0 None -32 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1021/jm060262x
CHEMBL425622 172821 0 None -32 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 4 1 4 5.2 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C(C)C 10.1021/jm060262x
CHEMBL1441214 46591 0 None - 1 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1476898 46591 0 None - 1 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
71454275 90823 0 None -41 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]UK 14.304 from human adrenergic alpha2A receptorDisplacement of [3H]UK 14.304 from human adrenergic alpha2A receptor
ChEMBL 293 3 1 3 3.0 CCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1 10.1021/jm300975f
CHEMBL2207493 90823 0 None -41 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]UK 14.304 from human adrenergic alpha2A receptorDisplacement of [3H]UK 14.304 from human adrenergic alpha2A receptor
ChEMBL 293 3 1 3 3.0 CCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1 10.1021/jm300975f
11221758 91392 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccccc1[N+](=O)[O-])C1=NCCN1 10.1021/jm0408215
CHEMBL222138 91392 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1ccccc1[N+](=O)[O-])C1=NCCN1 10.1021/jm0408215
90644716 119494 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 233 3 4 2 1.5 N=C(NCCO)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3289526 119494 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 233 3 4 2 1.5 N=C(NCCO)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3304535 119494 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 233 3 4 2 1.5 N=C(NCCO)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
16725934 154201 0 None -87 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL392992 154201 0 None -87 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 10.1016/j.bmcl.2006.12.094
44574077 185539 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468710 185539 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
136 10065 32 None -12 16 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
223 10065 32 None -12 16 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
643606 10065 32 None -12 16 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
CHEMBL10347 10065 32 None -12 16 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
3024499 182252 73 None 20 2 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccc(N2CCNCC2)n1 10.1021/jm00366a007
CHEMBL45773 182252 73 None 20 2 Bovine 7.8 pKi = 7.8 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccc(N2CCNCC2)n1 10.1021/jm00366a007
11140347 211312 1 None -2 6 Human 7.7 pKi = 7.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 211312 1 None -2 6 Human 7.7 pKi = 7.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44292381 108171 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 244 2 1 3 2.7 c1ccc([C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL297228 108171 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 244 2 1 3 2.7 c1ccc([C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
25142456 89181 2 None -89 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned adrenergic alpha 2A receptorBinding affinity to human cloned adrenergic alpha 2A receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None -89 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned adrenergic alpha 2A receptorBinding affinity to human cloned adrenergic alpha 2A receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
188249 46427 4 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL147463 46427 4 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL2022280 46427 4 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
73213195 111236 0 None -61 12 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 111236 0 None -61 12 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
164615845 191969 0 None -1 6 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
CHEMBL4857492 191969 0 None -1 6 Human 5.8 pKi = 5.8 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic 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
5198 26205 54 None - 1 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 nan
CHEMBL12948 26205 54 None - 1 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 nan
68712 107114 60 None -1 5 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
CHEMBL289480 107114 60 None -1 5 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/0960-894X(94)85032-1
57395663 77956 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.5 CC(Oc1ccccc1C(F)(F)F)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956193 77956 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.5 CC(Oc1ccccc1C(F)(F)F)C1=NCCN1 10.1016/j.bmc.2012.01.035
122065 196328 3 None -3630 8 Human 5.7 pKi = 5.7 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
CHEMBL51433 196328 3 None -3630 8 Human 5.7 pKi = 5.7 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
2247 7293 81 None -58 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -58 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -58 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -58 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -58 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
73213195 111236 0 None -61 12 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 111236 0 None -61 12 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
10379016 23264 2 None -1 3 Bovine 6.7 pKi = 6.7 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL123566 23264 2 None -1 3 Bovine 6.7 pKi = 6.7 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
3117 214620 103 None -2 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
135398737 7745 93 None -26 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
38 7745 93 None -26 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
722 7745 93 None -26 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
CHEMBL42 7745 93 None -26 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
DB00363 7745 93 None -26 90 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
10362866 89074 0 None -371 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
CHEMBL217203 89074 0 None -371 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
10474679 103952 0 None -288 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1021/jm060262x
CHEMBL268217 103952 0 None -288 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 4.0 CN1CCN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CC1(C)C 10.1021/jm060262x
44438168 100593 0 None -53 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 533 7 0 7 4.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)N4CCC(N5CCCC5)CC4)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL247665 100593 0 None -53 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 533 7 0 7 4.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)N4CCC(N5CCCC5)CC4)cc13)CC2 10.1016/j.bmcl.2006.12.094
44324900 213677 0 None -2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 423 6 0 7 2.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL90843 213677 0 None -2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 423 6 0 7 2.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
11043720 98947 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL242265 98947 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
11043720 98947 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL242265 98947 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
44289035 107290 0 None -977 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL291166 107290 0 None -977 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
90644714 119547 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 4 4 3 0.7 CN(C)c1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289527 119547 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 4 4 3 0.7 CN(C)c1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305464 119547 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 4 4 3 0.7 CN(C)c1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
155538461 179180 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 494 7 0 6 5.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(C(F)(F)F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4476557 179180 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 494 7 0 6 5.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(C(F)(F)F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
90644718 119537 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 5 5 3 1.0 CCNc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289525 119537 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 5 5 3 1.0 CCNc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305320 119537 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 222 5 5 3 1.0 CCNc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
1353 8692 93 None -190 85 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -190 85 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -190 85 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -190 85 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -190 85 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
16090601 89167 0 None -208 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1c(CO)nc2ccccc2c1Nc1ccc(N2CCN(C)[C@H](C)C2)cc1 10.1021/jm060262x
CHEMBL217254 89167 0 None -208 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1c(CO)nc2ccccc2c1Nc1ccc(N2CCN(C)[C@H](C)C2)cc1 10.1021/jm060262x
10873978 175265 0 None -4 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL435218 175265 0 None -4 5 Rat 5.7 pKi = 5.7 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
135398737 7745 93 None -10 90 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 7745 93 None -10 90 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 7745 93 None -10 90 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 7745 93 None -10 90 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 7745 93 None -10 90 Rat 7.7 pKi = 7.7 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
10106205 213916 1 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Alpha-2 adrenergic receptorBinding affinity towards Alpha-2 adrenergic receptor
ChEMBL 251 2 2 3 3.0 Cc1c(NC2=NCCN2)cccc1-c1ccccc1 10.1021/jm030030n
CHEMBL92221 213916 1 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Alpha-2 adrenergic receptorBinding affinity towards Alpha-2 adrenergic receptor
ChEMBL 251 2 2 3 3.0 Cc1c(NC2=NCCN2)cccc1-c1ccccc1 10.1021/jm030030n
12981870 64894 2 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 200 2 1 3 2.0 C1=NCC(Cc2cc3ccccc3o2)N1 10.1021/jm001040g
CHEMBL167644 64894 2 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 200 2 1 3 2.0 C1=NCC(Cc2cc3ccccc3o2)N1 10.1021/jm001040g
10465942 20317 0 None 1 3 Bovine 6.7 pKi = 6.7 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1193821 20317 0 None 1 3 Bovine 6.7 pKi = 6.7 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL545289 20317 0 None 1 3 Bovine 6.7 pKi = 6.7 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
16090596 89066 0 None -275 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL217177 89066 0 None -275 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1nc2c(C)cccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
21584368 206631 3 None -4 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 208 2 2 4 0.6 O=[N+]([O-])c1ccc2c(c1)CNC(CO)C2 10.1021/acs.jmedchem.0c01475
CHEMBL59441 206631 3 None -4 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 208 2 2 4 0.6 O=[N+]([O-])c1ccc2c(c1)CNC(CO)C2 10.1021/acs.jmedchem.0c01475
90644712 119527 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 5 4 3 1.0 CCOc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289528 119527 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 5 4 3 1.0 CCOc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305159 119527 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 223 5 4 3 1.0 CCOc1ccc(NC(=N)NCCO)cc1 10.1016/j.ejmech.2014.05.057
135398745 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
47 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
CHEMBL715 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
DB00334 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
162672516 189901 0 None -3 7 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4794963 189901 0 None -3 7 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
127036186 144192 0 None -6 19 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 144192 0 None -6 19 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
14004039 126339 3 None 5 2 Bovine 6.7 pKi = 6.7 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
CHEMBL346016 126339 3 None 5 2 Bovine 6.7 pKi = 6.7 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
12699315 83073 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 243 1 2 3 2.8 CC1CNC(Nc2c(Cl)cccc2Cl)=N1 10.1016/j.bmc.2012.06.008
CHEMBL2058631 83073 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 243 1 2 3 2.8 CC1CNC(Nc2c(Cl)cccc2Cl)=N1 10.1016/j.bmc.2012.06.008
14004039 126339 3 None 5 2 Bovine 6.7 pKi = 6.7 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
CHEMBL346016 126339 3 None 5 2 Bovine 6.7 pKi = 6.7 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 193 0 0 2 2.8 c1cc2c(s1)C1CCCCN1CC2 10.1021/jm00398a025
44288874 107872 0 None -1949 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL295001 107872 0 None -1949 7 Human 5.7 pKi = 5.7 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
11034737 211307 0 None 2 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 211307 0 None 2 6 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
14004032 126612 2 None 1 2 Bovine 5.7 pKi = 5.7 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL348538 126612 2 None 1 2 Bovine 5.7 pKi = 5.7 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
185076 193869 5 None 2 7 Human 8.7 pKi = 8.7 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm960359r
CHEMBL49137 193869 5 None 2 7 Human 8.7 pKi = 8.7 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm960359r
185076 193869 5 None 2 7 Human 8.7 pKi = 8.7 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm9605142
CHEMBL49137 193869 5 None 2 7 Human 8.7 pKi = 8.7 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1021/jm9605142
2142 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
4920903 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
502 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
5775 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
CHEMBL597 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
DB00692 9870 58 None 1 37 Bovine 8.7 pKi = 8.7 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00366a022
2142 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 9870 58 None -2 37 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
124 9755 47 None -4 32 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
2032 9755 47 None -4 32 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
4636 9755 47 None -4 32 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
CHEMBL762 9755 47 None -4 32 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
DB00935 9755 47 None -4 32 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/j.bmcl.2013.12.024
102 10899 48 None -5 49 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
3659 10899 48 None -5 49 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
8969 10899 48 None -5 49 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
CHEMBL15245 10899 48 None -5 49 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
DB01392 10899 48 None -5 49 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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 nan
218362 211579 5 None -1 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL75030 211579 5 None -1 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 216 1 1 3 2.0 c1ccc2c(c1)CCCC2NC1=NCCO1 10.1016/0960-894X(94)85032-1
73453 36389 24 None -3 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 36389 24 None -3 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
135440165 85720 0 None -23 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112985 85720 0 None -23 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
136019934 151308 0 None -7 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
CHEMBL390718 151308 0 None -7 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
9928332 103955 5 None -1 9 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/s0960-894x(03)00525-0
CHEMBL268258 103955 5 None -1 9 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/s0960-894x(03)00525-0
9928332 103955 5 None -1 9 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL268258 103955 5 None -1 9 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
10176567 109577 3 None 10 4 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm990569e
CHEMBL30534 109577 3 None 10 4 Rat 8.6 pKi = 8.6 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm990569e
44324765 118345 0 None -2 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL328114 118345 0 None -2 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
10176567 109577 3 None 10 4 Rat 8.6 pKi = 8.6 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm000128r
CHEMBL30534 109577 3 None 10 4 Rat 8.6 pKi = 8.6 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm000128r
44324765 118345 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL328114 118345 0 None -2 5 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
2142 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
4920903 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
502 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
5775 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
CHEMBL597 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
DB00692 9870 58 None -2 37 Human 8.6 pKi = 8.6 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
11959098 186315 56 None 79 2 Bovine 8.6 pKi = 8.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 211 1 0 3 1.5 CN1CCN(c2ncccc2Cl)CC1 10.1021/jm00366a007
CHEMBL47415 186315 56 None 79 2 Bovine 8.6 pKi = 8.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 211 1 0 3 1.5 CN1CCN(c2ncccc2Cl)CC1 10.1021/jm00366a007
2435 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
395 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
520 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
5386 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
CHEMBL844 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
DB00484 7509 100 None -2 12 Human 8.6 pKi = 8.6 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1021/jm9605142
3038495 7495 37 None -1 18 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2010.07.002
7625 7495 37 None -1 18 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2010.07.002
CHEMBL25236 7495 37 None -1 18 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2010.07.002
46934427 22400 0 None 3 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 481 11 1 5 4.5 COc1ccccc1N1CCN(CCCCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221594 22400 0 None 3 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 481 11 1 5 4.5 COc1ccccc1N1CCN(CCCCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
12203911 195062 22 None 54 2 Bovine 8.5 pKi = 8.5 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 255 1 0 3 1.6 CN1CCN(c2ncccc2Br)CC1 10.1021/jm00366a007
CHEMBL50017 195062 22 None 54 2 Bovine 8.5 pKi = 8.5 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 255 1 0 3 1.6 CN1CCN(c2ncccc2Br)CC1 10.1021/jm00366a007
9816063 109851 0 None 4 6 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
CHEMBL30739 109851 0 None 4 6 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
2216 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 10.1021/jm960359r
229 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 10.1021/jm960359r
7117 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 10.1021/jm960359r
CHEMBL647 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 10.1021/jm960359r
DB00964 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 10.1021/jm960359r
44330584 114896 0 None -1 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL319573 114896 0 None -1 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
10480357 214997 0 None -9 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL98541 214997 0 None -9 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
9816063 109851 0 None 4 6 Rat 8.5 pKi = 8.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm000128r
CHEMBL30739 109851 0 None 4 6 Rat 8.5 pKi = 8.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm000128r
44314198 111189 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
CHEMBL310335 111189 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCCC1NC1=NCCO1 10.1016/0960-894X(94)85032-1
9815707 108246 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL297752 108246 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 210 3 1 3 2.3 CCC[C@H]1CCCC[C@@H]1NC1=NCCO1 10.1021/jm9905256
134551 7146 27 None -3 21 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 7146 27 None -3 21 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 7146 27 None -3 21 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 7146 27 None -3 21 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
11224953 85709 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 459 6 1 5 3.3 CCNC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
CHEMBL2112973 85709 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 459 6 1 5 3.3 CCNC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
135499867 85716 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 388 5 1 5 3.2 C(=C/c1ccccc1)\CN1CCN(C[C@@H]2ON=C3c4ccccc4NC[C@H]32)CC1 10.1021/jm049619s
CHEMBL2112981 85716 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 388 5 1 5 3.2 C(=C/c1ccccc1)\CN1CCN(C[C@@H]2ON=C3c4ccccc4NC[C@H]32)CC1 10.1021/jm049619s
1816 9318 102 None -51 18 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
4205 9318 102 None -51 18 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
7241 9318 102 None -51 18 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
CHEMBL654 9318 102 None -51 18 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
DB00370 9318 102 None -51 18 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
49836303 25344 1 None -3 4 Human 7.7 pKi = 7.7 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276220 25344 1 None -3 4 Human 7.7 pKi = 7.7 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
2803 7742 58 None -1 19 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.ejmech.2014.05.057
516 7742 58 None -1 19 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.ejmech.2014.05.057
704 7742 58 None -1 19 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.ejmech.2014.05.057
CHEMBL134 7742 58 None -1 19 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.ejmech.2014.05.057
DB00575 7742 58 None -1 19 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.ejmech.2014.05.057
49836303 25344 1 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276220 25344 1 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
10848826 195659 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 258 3 1 3 2.8 c1ccc(C[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL50719 195659 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 258 3 1 3 2.8 c1ccc(C[C@H]2CCCC[C@@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL508338 195745 0 None -6 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
14004032 126612 2 None 1 2 Bovine 5.7 pKi = 5.7 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL348538 126612 2 None 1 2 Bovine 5.7 pKi = 5.7 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 188 0 0 2 2.2 c1cnc2c(c1)CCN1CCCCC21 10.1021/jm00398a025
44415672 86949 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 86949 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
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
11057 182928 23 None -1 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 182928 23 None -1 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 182928 23 None -1 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 182928 23 None -1 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44574106 185205 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466012 185205 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
135398745 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -93 65 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1201549 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 7384 24 None -33 20 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
11750482 154199 0 None -25 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL392991 154199 0 None -25 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 10.1016/j.bmcl.2006.12.094
12909388 67830 0 None -14 2 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 303 0 0 3 3.4 CN1CCC(=C2c3cc(C#N)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL176365 67830 0 None -14 2 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 303 0 0 3 3.4 CN1CCC(=C2c3cc(C#N)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
3598 194600 76 None -2 7 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 194600 76 None -2 7 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
44579187 196458 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 513 8 1 8 3.3 N#Cc1cccc(Oc2ncccc2C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)c1 10.1016/j.bmcl.2008.08.055
CHEMBL515331 196458 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 513 8 1 8 3.3 N#Cc1cccc(Oc2ncccc2C(=O)NCCN2CCCN(CC3COc4ccccc4O3)CC2)c1 10.1016/j.bmcl.2008.08.055
132060733 168903 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 294 3 0 3 3.0 c1ccc(CN2Cc3ccc(N4CCOCC4)cc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4161503 168903 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 294 3 0 3 3.0 c1ccc(CN2Cc3ccc(N4CCOCC4)cc3C2)cc1 10.1016/j.ejmech.2018.02.024
11801828 213323 0 None -128 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL88628 213323 0 None -128 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 606 9 3 6 5.0 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
124 9755 47 None -16 32 Pig 7.7 pKi = 7.7 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
2032 9755 47 None -16 32 Pig 7.7 pKi = 7.7 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
4636 9755 47 None -16 32 Pig 7.7 pKi = 7.7 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
CHEMBL762 9755 47 None -16 32 Pig 7.7 pKi = 7.7 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
DB00935 9755 47 None -16 32 Pig 7.7 pKi = 7.7 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm00018a001
123920 106930 41 None 309 2 Rat 7.7 pKi = 7.7 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 201 0 1 1 2.6 Clc1ccc2c(c1Cl)CNCC2 10.1021/jm0205752
CHEMBL287837 106930 41 None 309 2 Rat 7.7 pKi = 7.7 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 201 0 1 1 2.6 Clc1ccc2c(c1Cl)CNCC2 10.1021/jm0205752
4209 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
4893 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
503 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
5385 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
CHEMBL2 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
DB00457 9937 75 None -1380 33 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00010a001
13141182 137671 1 None -10 2 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 354 0 0 2 4.7 CN1CCC(=C2c3cc(Br)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368578 137671 1 None -10 2 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 354 0 0 2 4.7 CN1CCC(=C2c3cc(Br)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
10490084 211737 1 None 7 3 Human 6.7 pKi = 6.7 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 237 2 2 2 2.9 Brc1ccccc1Nc1ncc[nH]1 10.1021/jm9605142
CHEMBL76457 211737 1 None 7 3 Human 6.7 pKi = 6.7 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 237 2 2 2 2.9 Brc1ccccc1Nc1ncc[nH]1 10.1021/jm9605142
44574045 196065 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
CHEMBL512062 196065 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
50878551 97520 61 None -5 18 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 97520 61 None -5 18 Human 6.7 pKi = 6.7 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
24906197 194445 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL495097 194445 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 323 7 1 5 3.0 CC(Oc1ccccc1/C=N/OCc1ccccc1)C1=NCCN1 10.1021/jm800250z
90644704 119492 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 4 2 3 2.1 CN(C)c1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289532 119492 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 4 2 3 2.1 CN(C)c1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304530 119492 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 258 4 2 3 2.1 CN(C)c1ccc(/N=C(/N)NCc2ccco2)cc1 10.1016/j.ejmech.2014.05.057
4209 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 9937 75 None -1380 33 Human 5.7 pKi = 5.7 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
10793665 113729 0 None -1202 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 597 9 2 5 7.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm980077m
CHEMBL314960 113729 0 None -1202 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 597 9 2 5 7.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)cc1 10.1021/jm980077m
1549008 212459 85 None - 1 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 nan
CHEMBL822 212459 85 None - 1 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 nan
44438161 153919 0 None -22 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 543 10 1 7 5.0 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4cccc(C(=O)NCCN(C)C)c4)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL392771 153919 0 None -22 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 543 10 1 7 5.0 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4cccc(C(=O)NCCN(C)C)c4)cc13)CC2 10.1016/j.bmcl.2006.12.094
2520 210787 70 None -6 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 210787 70 None -6 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 210787 70 None -6 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
12488 8438 56 None -6 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 8438 56 None -6 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 8438 56 None -6 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 8438 56 None -6 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
11098175 210949 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 210949 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
10841190 113819 0 None -309 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 2 6 6.5 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1021/jm980077m
CHEMBL315538 113819 0 None -309 6 Human 5.7 pKi = 5.7 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 2 6 6.5 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(OC)cc1 10.1021/jm980077m
90644740 119507 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 4 3 3 2.6 CCNc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289549 119507 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 4 3 3 2.6 CCNc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304693 119507 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 270 4 3 3 2.6 CCNc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL1200633 215379 3 None -7 8 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
133 9274 52 None -23 43 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 9274 52 None -23 43 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 9274 52 None -23 43 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 9274 52 None -23 43 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 9274 52 None -23 43 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
44330679 215053 0 None -10 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 464 7 0 8 2.9 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccnc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL98889 215053 0 None -10 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 464 7 0 8 2.9 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccnc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44324859 118389 0 None -4 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 461 6 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CC4=Cc5ccccc5C4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL328377 118389 0 None -4 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 461 6 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CC4=Cc5ccccc5C4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44549156 25342 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276218 25342 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
57345626 77955 2 None 6 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
CHEMBL1956192 77955 2 None 6 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1021/ml400232p
57345626 77955 2 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956192 77955 2 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 268 3 1 3 2.2 CC(Oc1ccccc1Br)C1=NCCN1 10.1016/j.bmc.2012.01.035
45487956 205146 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 230 3 1 3 2.6 CC(OC1=NCCN1)c1ccccc1C1CC1 10.1021/jm901262f
CHEMBL576623 205146 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 230 3 1 3 2.6 CC(OC1=NCCN1)c1ccccc1C1CC1 10.1021/jm901262f
44549156 25342 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276218 25342 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 CC(Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
11347303 118157 0 None -1 5 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1ccc2c(c1)C(c1c[nH]cn1)CCC2 10.1021/jm030551a
CHEMBL327116 118157 0 None -1 5 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 4 2 3 2.6 CCS(=O)(=O)Nc1ccc2c(c1)C(c1c[nH]cn1)CCC2 10.1021/jm030551a
44579185 188593 1 None -28 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
CHEMBL477816 188593 1 None -28 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
5288606 103959 26 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 259 0 1 1 1.9 Ic1ccc2c(c1)CNCC2 10.1021/jm0205752
CHEMBL26828 103959 26 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 259 0 1 1 1.9 Ic1ccc2c(c1)CNCC2 10.1021/jm0205752
16090602 89223 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 362 4 2 5 3.6 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1C 10.1021/jm060262x
CHEMBL217542 89223 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 362 4 2 5 3.6 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1C 10.1021/jm060262x
164618319 191372 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4848838 191372 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
10132386 103873 2 None -63 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1021/jm060262x
CHEMBL267464 103873 2 None -63 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 346 3 1 4 4.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1C 10.1021/jm060262x
155566702 182685 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 472 9 0 6 4.2 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CCc3ccc(F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4587003 182685 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 472 9 0 6 4.2 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CCc3ccc(F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
90644722 119491 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 4 3 2 3.5 CCOc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289523 119491 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 4 3 2 3.5 CCOc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304529 119491 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 4 3 2 3.5 CCOc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
49783209 24381 0 None -3890 26 Human 5.7 pKi = 5.7 Binding
Binding affinity to human adrenergic alpha2A receptorBinding affinity to human adrenergic alpha2A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -3890 26 Human 5.7 pKi = 5.7 Binding
Binding affinity to human adrenergic alpha2A receptorBinding affinity to human adrenergic alpha2A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
9906978 49485 2 None -165 12 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 49485 2 None -165 12 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
9837106 110934 2 None -8 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm990569e
CHEMBL30955 110934 2 None -8 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm990569e
9837106 110934 2 None 8 4 Rat 6.7 pKi = 6.7 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm000128r
CHEMBL30955 110934 2 None 8 4 Rat 6.7 pKi = 6.7 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm000128r
1443 8809 34 None -23 11 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
33625 8809 34 None -23 11 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
501 8809 34 None -23 11 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
CHEMBL279516 8809 34 None -23 11 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
DB08950 8809 34 None -23 11 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 10.1021/jm00018a001
2162 48288 100 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 48288 100 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
12909385 67203 1 None -7 2 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 276 0 0 2 4.0 CN1CCC(=C2c3ccccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL175154 67203 1 None -7 2 Bovine 6.7 pKi = 6.7 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 276 0 0 2 4.0 CN1CCC(=C2c3ccccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
135453290 140384 33 None -758 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]clonidine from cloned human adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]clonidine from cloned human adrenergic alpha2A receptor expressed in Sf9 cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 140384 33 None -758 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]clonidine from cloned human adrenergic alpha2A receptor expressed in Sf9 cellsDisplacement of [3H]clonidine from cloned human adrenergic alpha2A receptor expressed in Sf9 cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
21509921 111235 0 None -22 24 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 111235 0 None -22 24 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44288945 175694 0 None -575 7 Human 6.6 pKi = 6.6 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43860 175694 0 None -575 7 Human 6.6 pKi = 6.6 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
21509921 111235 0 None -22 24 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 111235 0 None -22 24 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
3080926 162374 21 None 10 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/acs.jmedchem.9b02080
CHEMBL404505 162374 21 None 10 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/acs.jmedchem.9b02080
44330571 170778 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C\c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL420830 170778 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C\c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
44330571 170778 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C\c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL420830 170778 0 None -2 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C\c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
9883506 77339 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 282 3 3 5 2.3 Cc1ccc(N(NC2=NCCN2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
CHEMBL194849 77339 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 282 3 3 5 2.3 Cc1ccc(N(NC2=NCCN2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
44371745 56063 0 None 11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL156336 56063 0 None 11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 218 4 1 3 2.0 CCc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
13123527 108567 3 None - 1 Bovine 6.6 pKi = 6.6 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 189 3 2 3 1.4 Cc1ccc(NCC2=NCCN2)cc1 10.1021/jm00366a022
CHEMBL300053 108567 3 None - 1 Bovine 6.6 pKi = 6.6 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 189 3 2 3 1.4 Cc1ccc(NCC2=NCCN2)cc1 10.1021/jm00366a022
13141184 172669 0 None -17 2 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 376 1 0 3 5.6 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL424967 172669 0 None -17 2 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 376 1 0 3 5.6 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
11198145 16587 2 None -85 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL113830 16587 2 None -85 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
16090597 148248 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1nc2c(C)ccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL384318 148248 0 None -5 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1nc2c(C)ccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
44328920 115418 0 None -199 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 705 14 3 7 5.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCC(F)(F)F)N1 10.1016/s0960-894x(99)00484-9
CHEMBL320736 115418 0 None -199 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 705 14 3 7 5.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCC(F)(F)F)N1 10.1016/s0960-894x(99)00484-9
44325028 213750 0 None -2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cccc5ccccc45)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL91297 213750 0 None -2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cccc5ccccc45)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44325079 213964 0 None -2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 437 7 0 7 2.7 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL92496 213964 0 None -2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 437 7 0 7 2.7 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
90644732 119495 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 1 2 3 1.0 CC1CN/C(=N/c2ccc3c(c2)OCO3)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3289545 119495 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 1 2 3 1.0 CC1CN/C(=N/c2ccc3c(c2)OCO3)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3304536 119495 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 219 1 2 3 1.0 CC1CN/C(=N/c2ccc3c(c2)OCO3)N1 10.1016/j.ejmech.2014.05.057
11080 35858 79 None 1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 35858 79 None 1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL4549667 220777 5 None -1 2 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000720a ADRA2ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000720a ADRA2A
ChEMBL None None None CN1C(=O)[C@@H](N2CCc3c(nn(Cc4ccccc4)c3Br)C2=O)COc2ccccc21 10.6019/CHEMBL5212743
CHEMBL4777443 220825 0 None -11 14 Human 6.6 pKi = 6.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a ADRA2ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a ADRA2A
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 10.6019/CHEMBL5212743
24906241 199596 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
CHEMBL522151 199596 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
24906200 199935 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
CHEMBL523048 199935 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 328 5 1 3 4.5 c1ccc(-c2ccccc2OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
135398737 7745 93 None -26 90 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
38 7745 93 None -26 90 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
722 7745 93 None -26 90 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
CHEMBL42 7745 93 None -26 90 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
DB00363 7745 93 None -26 90 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
126225 101751 5 None -10 7 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL25467 101751 5 None -10 7 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 263 1 0 2 4.2 C=Cc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
45487089 204419 0 None 10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 204 2 1 3 2.0 Cc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL570863 204419 0 None 10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 204 2 1 3 2.0 Cc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
10082076 20632 0 None 9 3 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195953 20632 0 None 9 3 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555637 20632 0 None 9 3 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
12841592 120271 2 None - 1 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 237 1 1 5 0.8 Clc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL331981 120271 2 None - 1 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 237 1 1 5 0.8 Clc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL538788 120271 2 None - 1 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 237 1 1 5 0.8 Clc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
9809007 179343 8 None -1905 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
CHEMBL448620 179343 8 None -1905 6 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1016/s0960-894x(99)00484-9
9884781 45448 1 None 1 5 Human 6.6 pKi = 6.6 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3ccc4c(c3)OCCO4)CC1)C2 10.1021/acs.jmedchem.7b00151
CHEMBL146556 45448 1 None 1 5 Human 6.6 pKi = 6.6 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3ccc4c(c3)OCCO4)CC1)C2 10.1021/acs.jmedchem.7b00151
11624518 207122 3 None -18 6 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL597601 207122 3 None -18 6 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
415628 214971 95 None -2 5 Bovine 7.6 pKi = 7.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00366a007
CHEMBL9841 214971 95 None -2 5 Bovine 7.6 pKi = 7.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00366a007
2389 10104 118 None -37 66 Rat 7.6 pKi = 7.6 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 10104 118 None -37 66 Rat 7.6 pKi = 7.6 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 10104 118 None -37 66 Rat 7.6 pKi = 7.6 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 10104 118 None -37 66 Rat 7.6 pKi = 7.6 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 10104 118 None -37 66 Rat 7.6 pKi = 7.6 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
10220232 106497 6 None 1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm990569e
CHEMBL284795 106497 6 None 1 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm990569e
6761 74574 19 None -6 18 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 74574 19 None -6 18 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44324765 118345 0 None -2 5 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL328114 118345 0 None -2 5 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
10220232 106497 6 None -1 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm000128r
CHEMBL284795 106497 6 None -1 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 230 1 1 2 3.5 Cc1sc(C)c2c1CCC=C2c1c[nH]cn1 10.1021/jm000128r
23292293 64941 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 244 2 1 2 3.0 Clc1cccc2ccc(CC3CN=CN3)cc12 10.1021/jm001040g
CHEMBL168168 64941 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 244 2 1 2 3.0 Clc1cccc2ccc(CC3CN=CN3)cc12 10.1021/jm001040g
44314200 109729 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
CHEMBL306377 109729 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 230 1 1 3 2.4 c1ccc2c(c1)CCCC2NC1=NCCCO1 10.1016/0960-894X(94)85032-1
11948707 172946 0 None -616 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to alpha 2A adrenergic receptor by radioligand binding assayBinding affinity to alpha 2A adrenergic receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 172946 0 None -616 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to alpha 2A adrenergic receptor by radioligand binding assayBinding affinity to alpha 2A adrenergic receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
11393666 199765 0 None -6456 19 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 199765 0 None -6456 19 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 199765 0 None -6456 19 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A 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
44401194 78070 0 None -33 7 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL195706 78070 0 None -33 7 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
9815610 106709 19 None -13 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm990569e
CHEMBL286246 106709 19 None -13 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm990569e
9815610 106709 19 None 13 4 Rat 6.6 pKi = 6.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm000128r
CHEMBL286246 106709 19 None 13 4 Rat 6.6 pKi = 6.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2ccsc2CC1 10.1021/jm000128r
5280953 104137 109 None -3 8 Human 5.6 pKi = 5.6 Binding
Binding affinity towards alpha-2A-Adrenergic receptorBinding affinity towards alpha-2A-Adrenergic receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
CHEMBL269538 104137 109 None -3 8 Human 5.6 pKi = 5.6 Binding
Binding affinity towards alpha-2A-Adrenergic receptorBinding affinity towards alpha-2A-Adrenergic receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
1752 52535 59 None -2 5 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
CHEMBL153062 52535 59 None -2 5 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1 nan
44438152 100383 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 10.1016/j.bmcl.2006.12.094
CHEMBL246639 100383 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 10.1016/j.bmcl.2006.12.094
2286 9957 51 None -13 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 9957 51 None -13 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 9957 51 None -13 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 9957 51 None -13 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 9957 51 None -13 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
24906242 194026 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2c(cccc2-c2ccccc2)O1 10.1021/jm800250z
CHEMBL492647 194026 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 310 3 1 5 2.5 COC1(C2=NCCN2)COc2c(cccc2-c2ccccc2)O1 10.1021/jm800250z
10073773 167902 16 None -1288 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 minsDisplacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4082473 167902 16 None -1288 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 minsDisplacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117187 167902 16 None -1288 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 minsDisplacement of [3H] MK-912 from human adrenergic alpha 2A receptor expressed in HT29 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
10042547 83076 5 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 334 1 1 2 3.9 CC1CCC(Nc2ccc(I)cc2Cl)=N1 10.1016/j.bmc.2012.06.008
CHEMBL2058635 83076 5 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 334 1 1 2 3.9 CC1CCC(Nc2ccc(I)cc2Cl)=N1 10.1016/j.bmc.2012.06.008
155546767 180418 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 456 8 0 7 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(OC)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4534152 180418 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 456 8 0 7 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(OC)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL1458880 44624 0 None - 1 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
3778834 108097 78 None 144 2 Bovine 7.6 pKi = 7.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 208 2 1 5 0.4 O=[N+]([O-])c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL296653 108097 78 None 144 2 Bovine 7.6 pKi = 7.6 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 208 2 1 5 0.4 O=[N+]([O-])c1cccnc1N1CCNCC1 10.1021/jm00366a007
44324725 213596 0 None -13 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 451 8 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCCc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL90419 213596 0 None -13 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 451 8 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(CCCc4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
12114850 20020 0 None 57 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 704 5 6 6 4.2 O=C(NCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1191424 20020 0 None 57 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 704 5 6 6 4.2 O=C(NCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL542520 20020 0 None 57 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 704 5 6 6 4.2 O=C(NCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
44269122 104885 2 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL273485 104885 2 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm800250z
45487144 204480 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 190 2 1 3 1.7 CC(OC1=NCCN1)c1ccccc1 10.1021/jm901262f
CHEMBL571314 204480 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 190 2 1 3 1.7 CC(OC1=NCCN1)c1ccccc1 10.1021/jm901262f
44269122 104885 2 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL273485 104885 2 None 6 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 190 3 1 3 1.5 CC(Oc1ccccc1)C1=NCCN1 10.1021/jm100977d
146025727 178464 0 None -97 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None -97 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK 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
90644746 119499 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 265 2 3 1 4.0 N=C(Nc1ccccc1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3289521 119499 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 265 2 3 1 4.0 N=C(Nc1ccccc1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3304553 119499 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 265 2 3 1 4.0 N=C(Nc1ccccc1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
90644734 119496 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 4 2 3 2.6 CCOc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289546 119496 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 4 2 3 2.6 CCOc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304537 119496 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 271 4 2 3 2.6 CCOc1ccc(/N=C2/NCC(c3ccco3)N2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL4576555 220796 5 None -2 19 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
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
44312198 211368 0 None 1 4 Human 4.6 pKi = 4.6 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL73164 211368 0 None 1 4 Human 4.6 pKi = 4.6 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 292 1 1 5 2.2 Brc1c(NC2=NCCO2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL4576555 220796 5 None -2 19 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
CHEMBL4576555 220796 5 None -2 19 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a ADRA2ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000705a ADRA2A
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
9926143 120303 1 None -467 4 Rat 5.6 pKi = 5.6 Binding
Compound was tested for binding affinity using [3H]prazosin against Alpha-1 adrenergic receptorCompound was tested for binding affinity using [3H]prazosin against Alpha-1 adrenergic receptor
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 120303 1 None -467 4 Rat 5.6 pKi = 5.6 Binding
Compound was tested for binding affinity using [3H]prazosin against Alpha-1 adrenergic receptorCompound was tested for binding affinity using [3H]prazosin against Alpha-1 adrenergic receptor
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
44401041 77262 0 None -63 7 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL194659 77262 0 None -63 7 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
3080926 162374 21 None 10 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/ml400232p
CHEMBL404505 162374 21 None 10 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 186 1 1 3 1.8 c1ccc2oc(C3=NCCN3)cc2c1 10.1021/ml400232p
44579186 188755 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 474 8 1 7 3.1 O=C(NCCN1CCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
CHEMBL478026 188755 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 474 8 1 7 3.1 O=C(NCCN1CCN(CC2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
9815633 106411 3 None -6 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
CHEMBL284213 106411 3 None -6 6 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm990569e
9815633 106411 3 None 6 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm000128r
CHEMBL284213 106411 3 None 6 6 Rat 7.6 pKi = 7.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 204 1 1 2 2.9 c1nc(C2CCCc3sccc32)c[nH]1 10.1021/jm000128r
11346584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
CHEMBL374584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm061487a
11346584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL374584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm0408215
11346584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL374584 143762 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
10266538 123749 2 None 1 2 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 295 1 0 5 1.2 CN1CCN(c2ncc(Br)n3ccnc23)CC1 10.1021/jm00099a012
CHEMBL338704 123749 2 None 1 2 Bovine 6.6 pKi = 6.6 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 295 1 0 5 1.2 CN1CCN(c2ncc(Br)n3ccnc23)CC1 10.1021/jm00099a012
1971 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 9641 38 None -8 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
9828476 213703 0 None -1202 6 Human 6.6 pKi = 6.6 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 532 9 2 7 5.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL91022 213703 0 None -1202 6 Human 6.6 pKi = 6.6 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 532 9 2 7 5.2 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
162265 209053 22 None -12 44 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
4786 209053 22 None -12 44 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
CHEMBL61006 209053 22 None -12 44 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 10.1021/jm030551a
73346042 98609 5 None -27542 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 98609 5 None -27542 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
4211 64596 83 None -1 4 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 64596 83 None -1 4 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
1028 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 7079 71 None -48 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
10176567 109577 3 None -10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm990569e
CHEMBL30534 109577 3 None -10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm990569e
10176567 109577 3 None 10 4 Rat 6.6 pKi = 6.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm000128r
CHEMBL30534 109577 3 None 10 4 Rat 6.6 pKi = 6.6 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 1 1 2 3.3 c1cc(-c2c[nH]cn2)c2ccsc2c1 10.1021/jm000128r
126720252 171454 0 None 12 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 171454 0 None 12 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK 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
16655023 114218 2 None -5 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
CHEMBL318235 114218 2 None -5 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
44292232 108098 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
CHEMBL296660 108098 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 222 3 1 3 2.2 CCC[C@H]1C2CCC(C2)[C@H]1NC1=NCCO1 10.1021/jm9905256
2389 10104 118 None -77 66 Human 7.6 pKi = 7.6 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
5073 10104 118 None -77 66 Human 7.6 pKi = 7.6 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
96 10104 118 None -77 66 Human 7.6 pKi = 7.6 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
CHEMBL85 10104 118 None -77 66 Human 7.6 pKi = 7.6 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
DB00734 10104 118 None -77 66 Human 7.6 pKi = 7.6 Binding
Binding affinity to alpha2 adrenergic receptor (unknown origin)Binding affinity to alpha2 adrenergic receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
57345625 77954 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956191 77954 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 224 3 1 3 2.1 CC(Oc1ccccc1Cl)C1=NCCN1 10.1016/j.bmc.2012.01.035
44574105 185587 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL469127 185587 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
24906202 193996 0 None 5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
CHEMBL492444 193996 0 None 5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
11380133 176146 0 None 5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccncc1)C1=NCCN1 10.1021/jm0408215
CHEMBL442045 176146 0 None 5 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 1 4 2.5 CC(Oc1ccccc1-c1ccncc1)C1=NCCN1 10.1021/jm0408215
44456400 19606 0 None -1 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 19606 0 None -1 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 19606 0 None -1 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 19606 0 None -1 10 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
13091268 84999 0 None -3090 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 84999 0 None -3090 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
24906159 194184 12 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
CHEMBL493675 194184 12 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 233 4 2 5 1.3 CC(Oc1ccccc1/C=N/O)C1=NCCN1 10.1021/jm800250z
11203101 78458 0 None -44 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
ChEMBL 515 7 3 5 4.1 O=C(CCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)OCc1ccccc1 10.1016/j.bmcl.2005.03.116
CHEMBL196451 78458 0 None -44 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-2a adrenergic receptorIn vitro binding affinity towards alpha-2a adrenergic receptor
ChEMBL 515 7 3 5 4.1 O=C(CCCNC(=O)[C@@H]1C2C[C@H]3c4[nH]c5ccccc5c4CCN3C[C@@H]2CC[C@@H]1O)OCc1ccccc1 10.1016/j.bmcl.2005.03.116
11811395 211480 0 None -2 4 Human 5.5 pKi = 5.5 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74071 211480 0 None -2 4 Human 5.5 pKi = 5.5 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
11777109 123745 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 254 0 1 2 2.9 Clc1cc(Cl)c2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
CHEMBL338683 123745 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 254 0 1 2 2.9 Clc1cc(Cl)c2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
9837106 110934 2 None 8 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm990569e
CHEMBL30955 110934 2 None 8 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm990569e
44330427 170154 0 None -4 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccc(F)c4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL419336 170154 0 None -4 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4cccc(F)c4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
9837106 110934 2 None 8 4 Rat 8.5 pKi = 8.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm000128r
CHEMBL30955 110934 2 None 8 4 Rat 8.5 pKi = 8.5 Binding
In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidineIn vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
ChEMBL 202 1 1 2 2.8 C1=C(c2c[nH]cn2)c2sccc2CC1 10.1021/jm000128r
102 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
3659 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
8969 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
CHEMBL15245 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
DB01392 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 minsDisplacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
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 10.1016/j.bmcl.2013.01.025
16655023 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
CHEMBL318235 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
102 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
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 10.1021/jm990277d
3659 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
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 10.1021/jm990277d
8969 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
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 10.1021/jm990277d
CHEMBL15245 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
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 10.1021/jm990277d
DB01392 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
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 10.1021/jm990277d
102 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
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 10.1021/acs.jmedchem.9b01465
3659 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
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 10.1021/acs.jmedchem.9b01465
8969 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
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 10.1021/acs.jmedchem.9b01465
CHEMBL15245 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
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 10.1021/acs.jmedchem.9b01465
DB01392 10899 48 None -5 49 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
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 10.1021/acs.jmedchem.9b01465
12576 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm001040g
71310 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm001040g
CHEMBL353972 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm001040g
DB11481 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 10.1021/jm001040g
10585356 127388 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 1 1 2 2.2 C1=NC[C@@H](C2C[C@@]23CCc2ccccc2C3)N1 10.1021/jm001040g
135433755 127388 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 1 1 2 2.2 C1=NC[C@@H](C2C[C@@]23CCc2ccccc2C3)N1 10.1021/jm001040g
CHEMBL354611 127388 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 1 1 2 2.2 C1=NC[C@@H](C2C[C@@]23CCc2ccccc2C3)N1 10.1021/jm001040g
78114676 176620 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 402 6 0 6 3.3 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4439953 176620 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 402 6 0 6 3.3 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
13123529 108640 0 None - 1 Bovine 8.5 pKi = 8.5 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 203 3 1 3 1.4 Cc1ccc(N(C)CC2=NCCN2)cc1 10.1021/jm00366a022
CHEMBL300628 108640 0 None - 1 Bovine 8.5 pKi = 8.5 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 203 3 1 3 1.4 Cc1ccc(N(C)CC2=NCCN2)cc1 10.1021/jm00366a022
49781006 24012 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 240 3 1 2 2.9 CCO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256565 24012 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 240 3 1 2 2.9 CCO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
136 10065 32 None -12 16 Bovine 8.5 pKi = 8.5 Binding
Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pineal
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 10.1021/jm00018a001
223 10065 32 None -12 16 Bovine 8.5 pKi = 8.5 Binding
Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pineal
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 10.1021/jm00018a001
643606 10065 32 None -12 16 Bovine 8.5 pKi = 8.5 Binding
Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pineal
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 10.1021/jm00018a001
CHEMBL10347 10065 32 None -12 16 Bovine 8.5 pKi = 8.5 Binding
Compound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]rauwolscine to Alpha-2 adrenergic receptor in bovine pineal
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 10.1021/jm00018a001
16655023 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
CHEMBL318235 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
16655023 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL318235 114218 2 None -5 7 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
499 10849 18 None -13 14 Human 8.5 pKi = 8.5 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 10849 18 None -13 14 Human 8.5 pKi = 8.5 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 10849 18 None -13 14 Human 8.5 pKi = 8.5 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
2389 10104 118 None -77 66 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 10104 118 None -77 66 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 10104 118 None -77 66 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 10104 118 None -77 66 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 10104 118 None -77 66 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
2803 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
516 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
704 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
CHEMBL134 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
DB00575 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960012o
2803 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
516 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
704 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
CHEMBL134 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
DB00575 7742 58 None -1 19 Human 8.4 pKi = 8.4 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm960359r
49781887 23916 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
CHEMBL1255617 23916 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 222 1 1 1 2.9 c1ccc2c(c1)[C@H]1C[C@@]1(c1c[nH]cn1)C21CC1 10.1021/jm1006269
9990389 127210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 200 2 1 2 1.8 C1=NCC(CC2Cc3ccccc3C2)N1 10.1021/jm001040g
CHEMBL353843 127210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 200 2 1 2 1.8 C1=NCC(CC2Cc3ccccc3C2)N1 10.1021/jm001040g
49781007 24013 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 254 4 1 2 3.3 CCCO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256566 24013 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 254 4 1 2 3.3 CCCO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
240 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
2769 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
44279790 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
660 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
CHEMBL1729 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
CHEMBL560739 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
DB00604 7731 43 None -3 25 Rat 7.5 pKi = 7.5 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00013a009
44324972 170151 0 None -2 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL419316 170151 0 None -2 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
9971924 191005 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
CHEMBL48341 191005 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscineInhibitory constant against human Alpha-2A adrenergic receptor expressed in LM(tk-) cells using [3H]rauwolscine
ChEMBL 298 5 1 3 3.4 c1ccc(CCC[C@H]2C3CCC(C3)[C@H]2NC2=NCCO2)cc1 10.1021/jm9905256
13123531 195020 0 None - 1 Bovine 6.5 pKi = 6.5 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 217 4 1 3 1.8 CCN(CC1=NCCN1)c1ccc(C)cc1 10.1021/jm00366a022
CHEMBL49953 195020 0 None - 1 Bovine 6.5 pKi = 6.5 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 217 4 1 3 1.8 CCN(CC1=NCCN1)c1ccc(C)cc1 10.1021/jm00366a022
9953974 84608 0 None -24 3 Human 5.5 pKi = 5.5 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
CHEMBL2092927 84608 0 None -24 3 Human 5.5 pKi = 5.5 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
7059292 83075 7 None -3 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 194 1 1 2 2.9 Clc1ccccc1NC1=NCCC1 10.1016/j.bmc.2012.06.008
CHEMBL2058633 83075 7 None -3 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 194 1 1 2 2.9 Clc1ccccc1NC1=NCCC1 10.1016/j.bmc.2012.06.008
9894818 105701 0 None -83 7 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 105701 0 None -83 7 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
44401042 131607 0 None -81 9 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL364270 131607 0 None -81 9 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
11225732 100432 0 None -16 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL246852 100432 0 None -16 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 10.1016/j.bmcl.2006.12.094
10198248 194228 40 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL49395 194228 40 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 213 1 2 5 1.0 c1cnc2cc(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
11199581 143337 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccccc1O)C1=NCCN1 10.1021/jm0408215
CHEMBL373830 143337 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccccc1O)C1=NCCN1 10.1021/jm0408215
9944467 16023 0 None -1 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 309 2 2 2 3.4 O=C(Nc1cccc2c1CCCC2c1c[nH]cn1)C(F)(F)F 10.1021/jm030551a
CHEMBL110751 16023 0 None -1 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 309 2 2 2 3.4 O=C(Nc1cccc2c1CCCC2c1c[nH]cn1)C(F)(F)F 10.1021/jm030551a
9794524 211622 2 None 10 3 Human 7.5 pKi = 7.5 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 225 2 2 4 2.4 Cc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
CHEMBL75491 211622 2 None 10 3 Human 7.5 pKi = 7.5 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 225 2 2 4 2.4 Cc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
10946567 23241 0 None -25 6 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
CHEMBL123448 23241 0 None -25 6 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 265 1 0 2 4.1 CCc1sc2ccc(Cl)c3c2c1CN(C)CC3 10.1021/jm00019a001
15463615 127142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 246 2 1 2 3.1 Clc1cccc2c1C=C(CC1CN=CN1)CC2 10.1021/jm001040g
CHEMBL353200 127142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 246 2 1 2 3.1 Clc1cccc2c1C=C(CC1CN=CN1)CC2 10.1021/jm001040g
44371864 57915 0 None 8 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 246 5 1 3 2.6 CCc1cccc(CC)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL157955 57915 0 None 8 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 246 5 1 3 2.6 CCc1cccc(CC)c1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
13141183 168742 1 None -15 2 Bovine 6.5 pKi = 6.5 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 310 0 0 2 4.6 CN1CCC(=C2c3cc(Cl)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL415761 168742 1 None -15 2 Bovine 6.5 pKi = 6.5 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 310 0 0 2 4.6 CN1CCC(=C2c3cc(Cl)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
10045088 87363 0 None -407 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1021/jm060262x
CHEMBL214996 87363 0 None -407 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 376 4 2 5 3.9 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1CO 10.1021/jm060262x
16090631 89166 0 None -630 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 4 2 5 4.5 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C(C)O 10.1021/jm060262x
CHEMBL217253 89166 0 None -630 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 4 2 5 4.5 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C(C)O 10.1021/jm060262x
10632290 211525 5 None 2 3 Human 5.5 pKi = 5.5 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 211 2 2 4 2.1 c1c[nH]c(Nc2ccc3nccnc3c2)n1 10.1021/jm9605142
CHEMBL74449 211525 5 None 2 3 Human 5.5 pKi = 5.5 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 211 2 2 4 2.1 c1c[nH]c(Nc2ccc3nccnc3c2)n1 10.1021/jm9605142
3191 109635 97 None -8 25 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -8 25 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
122295 16640 7 None -9 9 Rat 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
CHEMBL114166 16640 7 None -9 9 Rat 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 10.1021/jm00018a001
72947315 99264 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
CHEMBL2431280 99264 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 232 5 1 4 1.6 c1ccc(OC2CC2)c(OCC2=NCCN2)c1 10.1021/ml400232p
44456400 19606 0 None -1 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 19606 0 None -1 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 19606 0 None -1 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 19606 0 None -1 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysisDisplacement of [3H]Rauwolscine from human recombinant alpha2A-adrenoceptor expressed in MDCK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
57400959 77963 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 268 4 1 5 0.9 CC(Oc1ccccc1S(C)(=O)=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956200 77963 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 268 4 1 5 0.9 CC(Oc1ccccc1S(C)(=O)=O)C1=NCCN1 10.1016/j.bmc.2012.01.035
10337773 108362 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL298612 108362 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
6424833 105948 101 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 178 1 1 3 1.2 O=[N+]([O-])c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2004.12.013
CHEMBL281289 105948 101 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 178 1 1 3 1.2 O=[N+]([O-])c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2004.12.013
10584556 214773 4 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 210 2 1 3 1.6 O=[N+]([O-])c1ccc2c(c1)CNC(CF)C2 10.1016/j.bmcl.2004.12.013
CHEMBL97282 214773 4 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 210 2 1 3 1.6 O=[N+]([O-])c1ccc2c(c1)CNC(CF)C2 10.1016/j.bmcl.2004.12.013
3930 8932 43 None -112 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
540335 8932 43 None -112 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
CHEMBL106525 8932 43 None -112 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 368 3 1 4 4.9 CN1CCN(CC1)c1ccc(cc1)Nc1c2ccccc2nc2c1cccc2 10.1021/jm060262x
132075278 169423 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 169423 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
44415689 145887 0 None -363 6 Human 6.5 pKi = 6.5 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 145887 0 None -363 6 Human 6.5 pKi = 6.5 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
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
11385652 85711 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 460 6 0 6 3.7 CCOC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
CHEMBL2112975 85711 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 460 6 0 6 3.7 CCOC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
118717248 121902 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 219 1 2 3 0.5 Fc1ccc2cnn(N=C3NCCN3)c2c1 10.1016/j.ejmech.2014.09.083
CHEMBL3343699 121902 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 219 1 2 3 0.5 Fc1ccc2cnn(N=C3NCCN3)c2c1 10.1016/j.ejmech.2014.09.083
4038180 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to Homo sapiens (human) alpha2A receptorBinding affinity to Homo sapiens (human) alpha2A receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
480 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to Homo sapiens (human) alpha2A receptorBinding affinity to Homo sapiens (human) alpha2A receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
CHEMBL109783 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to Homo sapiens (human) alpha2A receptorBinding affinity to Homo sapiens (human) alpha2A receptor
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1007/s00044-004-0020-z
4038180 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
480 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
CHEMBL109783 6992 14 None -3 8 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm030551a
11186227 91497 0 None 9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccc(O)cc1)C1=NCCN1 10.1021/jm0408215
CHEMBL222798 91497 0 None 9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 CC(Oc1ccccc1-c1ccc(O)cc1)C1=NCCN1 10.1021/jm0408215
13141187 137494 0 None -9 2 Bovine 6.5 pKi = 6.5 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 378 1 0 3 5.2 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368475 137494 0 None -9 2 Bovine 6.5 pKi = 6.5 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 378 1 0 3 5.2 CN1CCC(=C2c3cc(SC(F)(F)F)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
9809007 179343 8 None -1905 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL448620 179343 8 None -1905 6 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 608 10 2 7 5.6 COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
162658038 187925 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 530 10 5 13 0.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccc([N+](=O)[O-])cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4760727 187925 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 530 10 5 13 0.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCNCC2Cc3ccc([N+](=O)[O-])cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
70788951 33928 1 None -1 5 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
CHEMBL1366 33928 1 None -1 5 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL None None None None nan
90644726 119485 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 2 2 2 1.3 CC1CN/C(=N/c2ccc(N(C)C)cc2)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3289542 119485 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 2 2 2 1.3 CC1CN/C(=N/c2ccc(N(C)C)cc2)N1 10.1016/j.ejmech.2014.05.057
CHEMBL3304469 119485 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 218 2 2 2 1.3 CC1CN/C(=N/c2ccc(N(C)C)cc2)N1 10.1016/j.ejmech.2014.05.057
155539605 179624 0 None -14 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] NECA from human adrenergic alpha 2A receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H] NECA from human adrenergic alpha 2A receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 179624 0 None -14 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] NECA from human adrenergic alpha 2A receptor expressed in MDCK cells by radioligand binding assayDisplacement of [3H] NECA from human adrenergic alpha 2A receptor expressed in MDCK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
8447 195728 84 None -4 13 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 195728 84 None -4 13 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
11199593 143977 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 1 3 3.8 CC(Sc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL374954 143977 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 282 4 1 3 3.8 CC(Sc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
44288769 107925 0 None -3090 7 Human 5.5 pKi = 5.5 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL295395 107925 0 None -3090 7 Human 5.5 pKi = 5.5 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
10176433 27420 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 186 0 1 2 1.5 C1=NCC2(CCc3ccccc3C2)N1 10.1021/jm00020a021
CHEMBL130853 27420 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 186 0 1 2 1.5 C1=NCC2(CCc3ccccc3C2)N1 10.1021/jm00020a021
135398737 7745 93 None -26 90 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 7745 93 None -26 90 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 7745 93 None -26 90 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 7745 93 None -26 90 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 7745 93 None -26 90 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44325027 213853 0 None -1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 474 6 0 8 3.2 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cnc5ccccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL91824 213853 0 None -1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 474 6 0 8 3.2 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cnc5ccccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
45487958 205170 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 190 2 1 3 1.5 Cc1ccccc1COC1=NCCN1 10.1021/jm901262f
CHEMBL576819 205170 0 None 11 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 190 2 1 3 1.5 Cc1ccccc1COC1=NCCN1 10.1021/jm901262f
10376607 20132 0 None 1 2 Bovine 6.5 pKi = 6.5 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
CHEMBL1192423 20132 0 None 1 2 Bovine 6.5 pKi = 6.5 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
CHEMBL543653 20132 0 None 1 2 Bovine 6.5 pKi = 6.5 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
10332138 16331 3 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 246 1 1 3 2.2 O=[N+]([O-])c1ccc2c(c1)CNC(C(F)(F)F)C2 10.1016/j.bmcl.2004.12.013
CHEMBL112351 16331 3 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 246 1 1 3 2.2 O=[N+]([O-])c1ccc2c(c1)CNC(C(F)(F)F)C2 10.1016/j.bmcl.2004.12.013
5226 103838 31 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 212 1 2 3 -0.0 NS(=O)(=O)c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2004.12.013
CHEMBL26717 103838 31 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 212 1 2 3 -0.0 NS(=O)(=O)c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2004.12.013
75201901 173204 19 None -251 24 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -251 24 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK 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
213 10625 55 None -10 43 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 10625 55 None -10 43 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 10625 55 None -10 43 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 10625 55 None -10 43 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 10625 55 None -10 43 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
9798466 141056 1 None -44 6 Rat 6.5 pKi = 6.5 Binding
In vivo binding affinity was evaluated against Alpha-1 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-1 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37170 141056 1 None -44 6 Rat 6.5 pKi = 6.5 Binding
In vivo binding affinity was evaluated against Alpha-1 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-1 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
14004037 60545 2 None 8 2 Bovine 6.5 pKi = 6.5 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL160388 60545 2 None 8 2 Bovine 6.5 pKi = 6.5 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
36324 33896 76 None - 1 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 293 4 0 2 4.9 Cc1ccc(/N=C/N(C)/C=N/c2ccc(C)cc2C)c(C)c1 nan
CHEMBL1365675 33896 76 None - 1 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 293 4 0 2 4.9 Cc1ccc(/N=C/N(C)/C=N/c2ccc(C)cc2C)c(C)c1 nan
14004037 60545 2 None 8 2 Bovine 6.5 pKi = 6.5 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
CHEMBL160388 60545 2 None 8 2 Bovine 6.5 pKi = 6.5 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 209 0 1 4 1.8 Nc1nc2c(s1)CCN1CCCCC21 10.1021/jm00398a025
46869265 23029 0 None -16 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 23029 0 None -16 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A 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
1548953 214458 27 None -1 17 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 214458 27 None -1 17 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
9895326 213806 0 None -331 6 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1021/jm980077m
CHEMBL91550 213806 0 None -331 6 Human 6.5 pKi = 6.5 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 621 12 3 6 5.7 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CC)N1 10.1021/jm980077m
57345628 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956195 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
57345628 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956195 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
68712 107114 60 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/j.bmc.2012.06.008
CHEMBL289480 107114 60 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1016/j.bmc.2012.06.008
57345628 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL1956195 77958 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 CC(Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
11608298 71850 4 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 228 2 1 3 1.9 O=[N+]([O-])c1ccc2c(c1)CNC(C(F)F)C2 10.1016/j.bmcl.2004.12.013
CHEMBL182376 71850 4 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 228 2 1 3 1.9 O=[N+]([O-])c1ccc2c(c1)CNC(C(F)F)C2 10.1016/j.bmcl.2004.12.013
16090634 89069 0 None -4 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 296 3 1 4 3.2 Cc1cncc(C)c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
CHEMBL217180 89069 0 None -4 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 296 3 1 4 3.2 Cc1cncc(C)c1Nc1ccc(N2CCN(C)CC2)cc1 10.1021/jm060262x
3072540 89190 13 None -97 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1021/jm060262x
CHEMBL217366 89190 13 None -97 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 382 4 1 4 5.3 CCN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1 10.1021/jm060262x
9817256 211017 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 211017 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44390749 70684 0 None -199 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/s0960-894x(99)00484-9
CHEMBL180561 70684 0 None -199 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 607 11 3 6 5.3 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1016/s0960-894x(99)00484-9
441383 27105 57 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
94459 71048 127 None 64 2 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
CHEMBL18094 71048 127 None 64 2 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 163 1 1 3 0.5 c1ccc(N2CCNCC2)nc1 10.1021/jm00366a007
3086326 211310 22 None 1 6 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL72753 211310 22 None 1 6 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 247 1 2 5 1.7 Clc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
11173568 91416 0 None 8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222371 91416 0 None 8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 281 4 2 4 2.7 CC(Oc1ccccc1-c1cccc(N)c1)C1=NCCN1 10.1021/jm0408215
10083242 20606 1 None 5 3 Bovine 6.4 pKi = 6.4 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195814 20606 1 None 5 3 Bovine 6.4 pKi = 6.4 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555391 20606 1 None 5 3 Bovine 6.4 pKi = 6.4 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
3584 10549 64 None -251 14 Human 5.4 pKi = 5.4 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
5401 10549 64 None -251 14 Human 5.4 pKi = 5.4 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
7302 10549 64 None -251 14 Human 5.4 pKi = 5.4 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
CHEMBL611 10549 64 None -251 14 Human 5.4 pKi = 5.4 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
DB01162 10549 64 None -251 14 Human 5.4 pKi = 5.4 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00018a001
9894818 105701 0 None -83 7 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL279436 105701 0 None -83 7 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 593 10 3 6 4.9 CC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
155547141 180398 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 518 9 0 7 5.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(Oc4ccccc4)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4533687 180398 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 518 9 0 7 5.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(Oc4ccccc4)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
56964794 80839 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022272 80839 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
12774559 196388 0 None - 1 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 191 3 3 4 0.8 Oc1cccc(NCC2=NCCN2)c1 10.1021/jm00366a022
CHEMBL51479 196388 0 None - 1 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 191 3 3 4 0.8 Oc1cccc(NCC2=NCCN2)c1 10.1021/jm00366a022
44574080 195725 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
CHEMBL508084 195725 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
44312036 211344 1 None -5 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
CHEMBL72995 211344 1 None -5 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 305 1 2 5 2.2 CC1CN=C(Nc2ccc3nccnc3c2Br)N1 10.1016/0960-894X(95)00391-6
57401787 78028 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 308 3 1 4 2.3 c1ccc(C2(c3ccccc3)COCC(C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956906 78028 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 308 3 1 4 2.3 c1ccc(C2(c3ccccc3)COCC(C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL5094181 222259 22 None -12 5 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
ChEMBL None None None O=C(NCCCn1ccnc1)c1cc2nc(-c3ccccc3)cc(-c3ccccc3)n2n1 10.6019/CHEMBL5058647
CHEMBL5094181 222259 22 None -12 5 Human 5.4 pKi = 5.4 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
ChEMBL None None None O=C(NCCCn1ccnc1)c1cc2nc(-c3ccccc3)cc(-c3ccccc3)n2n1 10.6019/CHEMBL5058647
90644724 119487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 3 3 2 3.2 CN(C)c1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289522 119487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 3 3 2 3.2 CN(C)c1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304483 119487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 3 3 2 3.2 CN(C)c1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
10221005 211101 0 None -5 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 211101 0 None -5 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
10682720 211941 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 259 3 2 3 3.8 COc1cc(C)c(Nc2ncc[nH]2)cc1C(C)(C)C 10.1021/jm9605142
CHEMBL78190 211941 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 259 3 2 3 3.8 COc1cc(C)c(Nc2ncc[nH]2)cc1C(C)(C)C 10.1021/jm9605142
12981867 127135 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 230 2 1 2 2.5 Fc1cccc2c1C=C(CC1CN=CN1)CC2 10.1021/jm001040g
CHEMBL353139 127135 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 230 2 1 2 2.5 Fc1cccc2c1C=C(CC1CN=CN1)CC2 10.1021/jm001040g
49836308 25556 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL1278084 25556 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
11651319 188407 27 None 17 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cnccc1N1CCNCC1 10.1021/jm00366a007
CHEMBL47740 188407 27 None 17 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cnccc1N1CCNCC1 10.1021/jm00366a007
21584368 206631 3 None 4 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 208 2 2 4 0.6 O=[N+]([O-])c1ccc2c(c1)CNC(CO)C2 10.1016/j.bmcl.2004.12.013
CHEMBL59441 206631 3 None 4 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 208 2 2 4 0.6 O=[N+]([O-])c1ccc2c(c1)CNC(CO)C2 10.1016/j.bmcl.2004.12.013
164585473 191341 0 None -7 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2a (unknown origin)Binding affinity to alpha2a (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 191341 0 None -7 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to alpha2a (unknown origin)Binding affinity to alpha2a (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
10841387 106394 0 None -112 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
CHEMBL284103 106394 0 None -112 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00019a001
11079593 210894 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70326 210894 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
10841387 106394 0 None -112 6 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL284103 106394 0 None -112 6 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 607 10 3 6 5.2 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
153287574 182026 0 None -5 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 182026 0 None -5 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
24906203 193997 0 None 2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
CHEMBL492445 193997 0 None 2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2ccc3c(c2)OC(C2=NCCN2)CO3)cc1 10.1021/jm800250z
57384051 78024 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@@H]2CO[C@@H](C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956902 78024 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@@H]2CO[C@@H](C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
136274357 85719 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 412 4 1 5 3.8 c1ccc2c(c1)NC[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm049619s
CHEMBL2112984 85719 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 412 4 1 5 3.8 c1ccc2c(c1)NC[C@@H]1C2=NO[C@H]1CN1CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm049619s
49864336 22389 0 None 11 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 453 9 1 5 3.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221545 22389 0 None 11 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 453 9 1 5 3.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
13507646 126392 0 None 3 2 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL346492 126392 0 None 3 2 Bovine 8.4 pKi = 8.4 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
13507646 126392 0 None 3 2 Bovine 8.4 pKi = 8.4 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL346492 126392 0 None 3 2 Bovine 8.4 pKi = 8.4 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 243 0 0 2 4.0 c1ccc2c3c(sc2c1)C1CCCCN1CC3 10.1021/jm00398a025
1593 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
30668 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
9868 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
CHEMBL17860 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
DB04948 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1016/j.bmc.2012.01.035
102 10899 48 None -15 49 Pig 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
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 10.1021/jm00018a001
3659 10899 48 None -15 49 Pig 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
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 10.1021/jm00018a001
8969 10899 48 None -15 49 Pig 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
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 10.1021/jm00018a001
CHEMBL15245 10899 48 None -15 49 Pig 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
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 10.1021/jm00018a001
DB01392 10899 48 None -15 49 Pig 8.4 pKi = 8.4 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
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 10.1021/jm00018a001
78114881 178560 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 288 5 0 6 0.9 CCOP(=O)(OCC)C1N=CC2C(=O)N(C)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4467833 178560 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 288 5 0 6 0.9 CCOP(=O)(OCC)C1N=CC2C(=O)N(C)C(=O)C21 10.1021/acs.jmedchem.9b02080
42273326 22388 0 None 3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 403 7 1 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221544 22388 0 None 3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 403 7 1 4 3.8 COc1ccccc1N1CCN(CCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
136 10065 32 None -3 16 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
223 10065 32 None -3 16 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
643606 10065 32 None -3 16 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
CHEMBL10347 10065 32 None -3 16 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
42388639 194833 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL497749 194833 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
11191321 69759 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 503 6 0 7 4.5 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)C(C)(C)C)cc4OC[C@H]32)CC1 10.1021/jm049619s
CHEMBL178588 69759 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 503 6 0 7 4.5 C/C(=C\c1ccccc1)CN1CCN(C[C@@H]2ON=C3c4ccc(OC(=O)C(C)(C)C)cc4OC[C@H]32)CC1 10.1021/jm049619s
2142 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
4920903 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
502 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
5775 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
CHEMBL597 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
DB00692 9870 58 None -2 37 Rat 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm00018a001
44404326 140302 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 283 3 2 5 2.7 Cc1ccc(N(NC2=NCCO2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
CHEMBL370818 140302 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 283 3 2 5 2.7 Cc1ccc(N(NC2=NCCO2)c2cccc(O)c2)cc1 10.1016/j.bmcl.2005.07.083
135 9310 43 None -4 56 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
1796 9310 43 None -4 56 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
4184 9310 43 None -4 56 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
CHEMBL6437 9310 43 None -4 56 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
DB06148 9310 43 None -4 56 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
9795515 211599 0 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 273 3 2 3 4.1 COc1c(C(C)(C)C)cc(C)c(Nc2ncc[nH]2)c1C 10.1021/jm9605142
CHEMBL75257 211599 0 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 273 3 2 3 4.1 COc1c(C(C)(C)C)cc(C)c(Nc2ncc[nH]2)c1C 10.1021/jm9605142
2585 7590 103 None -28 22 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 7590 103 None -28 22 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 7590 103 None -28 22 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 7590 103 None -28 22 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 7590 103 None -28 22 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
155515982 176789 0 None -1584 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None -1584 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
44438147 100264 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL246228 100264 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 10.1016/j.bmcl.2006.12.094
10032383 116887 0 None -389 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
136680387 116887 0 None -389 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL323579 116887 0 None -389 6 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 666 15 4 8 4.2 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN)N1 10.1016/s0960-894x(99)00484-9
73213196 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha 2A receptor (unknown origin)Binding affinity to adrenergic alpha 2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
CHEMBL3104093 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Binding affinity to adrenergic alpha 2A receptor (unknown origin)Binding affinity to adrenergic alpha 2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
73213196 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
44401105 76351 0 None -45 9 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193435 76351 0 None -45 9 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
73213196 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 111237 4 None -3 13 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
11109088 210959 0 None -8 6 Human 7.4 pKi = 7.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 210959 0 None -8 6 Human 7.4 pKi = 7.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
70695474 84447 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089156 84447 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
11173544 173040 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
CHEMBL426900 173040 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccc(-c2ccccc2OC(C)C2=NCCN2)cc1 10.1021/jm0408215
70695474 84447 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL2089156 84447 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 C[C@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
4209 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
4893 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
503 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
5385 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
CHEMBL2 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
DB00457 9937 75 None -794 33 Pig 5.4 pKi = 5.4 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm00018a001
9885114 126382 5 None -95 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 126382 5 None -95 12 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptorInhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
9885114 126382 5 None -95 12 Human 6.4 pKi = 6.4 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/acs.jmedchem.7b00151
CHEMBL346389 126382 5 None -95 12 Human 6.4 pKi = 6.4 Binding
Inhibition of alpha2A adrenergic receptor (unknown origin)Inhibition of alpha2A adrenergic receptor (unknown origin)
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/acs.jmedchem.7b00151
57326584 80840 0 None -4 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022273 80840 0 None -4 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
24906196 194025 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL492639 194025 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 261 6 1 5 1.8 CCO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
11500225 107978 61 None 38 2 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 289 1 1 3 1.1 Ic1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL295764 107978 61 None 38 2 Bovine 7.4 pKi = 7.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 289 1 1 3 1.1 Ic1cccnc1N1CCNCC1 10.1021/jm00366a007
44438167 155749 0 None -52 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL394218 155749 0 None -52 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 10.1016/j.bmcl.2006.12.094
1265 7729 60 None -75 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
6422124 7729 60 None -75 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
CHEMBL14638 7729 60 None -75 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
13123533 201688 1 None - 1 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 271 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)C2CCCCC2)cc1 10.1021/jm00366a022
CHEMBL541208 201688 1 None - 1 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 271 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)C2CCCCC2)cc1 10.1021/jm00366a022
62381256 119543 2 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 5 3 2 2.4 CCCNC(=N)Nc1ccc(OCC)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289535 119543 2 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 5 3 2 2.4 CCCNC(=N)Nc1ccc(OCC)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3305460 119543 2 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 221 5 3 2 2.4 CCCNC(=N)Nc1ccc(OCC)cc1 10.1016/j.ejmech.2014.05.057
13869716 167059 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 199 1 1 3 1.5 Cn1c(C2=NCCN2)cc2ccccc21 10.1021/acs.jmedchem.9b02080
CHEMBL41103 167059 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 199 1 1 3 1.5 Cn1c(C2=NCCN2)cc2ccccc21 10.1021/acs.jmedchem.9b02080
71456239 85715 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 385 5 0 4 3.8 C1=C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
CHEMBL2112979 85715 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 385 5 0 4 3.8 C1=C[C@@H]2C(=NO[C@H]2CN2CCN(C/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
13141185 67262 0 None -9 2 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 356 0 0 2 4.3 CN1CCC(=C2c3cc(Br)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL175508 67262 0 None -9 2 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 356 0 0 2 4.3 CN1CCC(=C2c3cc(Br)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
10401405 16449 16 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 279 0 1 1 3.0 FC(F)(F)C1Cc2ccc(Br)cc2CN1 10.1016/j.bmcl.2004.12.013
CHEMBL112964 16449 16 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 279 0 1 1 3.0 FC(F)(F)C1Cc2ccc(Br)cc2CN1 10.1016/j.bmcl.2004.12.013
2719 7704 74 None -4 11 Human 5.4 pKi = 5.4 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
5535 7704 74 None -4 11 Human 5.4 pKi = 5.4 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
607 7704 74 None -4 11 Human 5.4 pKi = 5.4 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
CHEMBL76 7704 74 None -4 11 Human 5.4 pKi = 5.4 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
DB00608 7704 74 None -4 11 Human 5.4 pKi = 5.4 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
45588795 119534 4 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 2 3 3 2.9 N=C(Nc1ccccc1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3289534 119534 4 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 2 3 3 2.9 N=C(Nc1ccccc1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
CHEMBL3305316 119534 4 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 255 2 3 3 2.9 N=C(Nc1ccccc1)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2014.05.057
4098 39279 30 None -13 11 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 39279 30 None -13 11 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 39279 30 None -13 11 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
49836304 25343 1 None 2 3 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1276219 25343 1 None 2 3 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/ml400232p
70693375 84446 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL2089155 84446 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml400232p
49836304 25343 1 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276219 25343 1 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 4 1 3 2.3 C[C@@H](Oc1ccccc1C1CC1)C1=NCCN1 10.1021/jm100977d
49836305 25348 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL1276248 25348 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 C[C@H](Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
70693375 84446 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
CHEMBL2089155 84446 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 244 5 1 3 2.4 C[C@@H](Oc1ccccc1CC1CC1)C1=NCCN1 10.1021/ml300064v
9944409 14385 0 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL108804 14385 0 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
44579272 193874 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 499 7 0 9 4.3 c1ccc(Oc2ncccc2-c2noc(CN3CCCN(CC4COc5ccccc5O4)CC3)n2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL491420 193874 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 499 7 0 9 4.3 c1ccc(Oc2ncccc2-c2noc(CN3CCCN(CC4COc5ccccc5O4)CC3)n2)cc1 10.1016/j.bmcl.2008.08.055
10397358 181766 44 None 70 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 178 1 2 4 0.1 Nc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL45665 181766 44 None 70 2 Bovine 6.4 pKi = 6.4 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 178 1 2 4 0.1 Nc1cccnc1N1CCNCC1 10.1021/jm00366a007
44579231 188346 0 None -28 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 396 6 1 6 1.7 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1 10.1016/j.bmcl.2008.08.055
CHEMBL476774 188346 0 None -28 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 396 6 1 6 1.7 O=C(NCCN1CCCN(CC2COc3ccccc3O2)CC1)c1cccnc1 10.1016/j.bmcl.2008.08.055
135418497 69813 0 None -1949 4 Human 6.4 pKi = 6.4 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
CHEMBL1788222 69813 0 None -1949 4 Human 6.4 pKi = 6.4 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4NC(=O)N32)CC1 10.1021/jm970159v
2812 11551 101 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
10531532 213873 0 None -51 6 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 594 9 2 7 6.0 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL91956 213873 0 None -51 6 Human 6.4 pKi = 6.4 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 594 9 2 7 6.0 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
10199335 211526 0 None -5 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 211526 0 None -5 4 Human 5.4 pKi = 5.4 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
49781008 24022 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 254 3 1 2 3.3 CC(C)O[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256608 24022 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 254 3 1 2 3.3 CC(C)O[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
11371902 148416 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
CHEMBL385310 148416 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm0408215
11371902 148416 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
CHEMBL385310 148416 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 272 4 1 4 3.2 CC(Oc1ccccc1-c1ccsc1)C1=NCCN1 10.1021/jm100977d
121938 148673 20 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 215 0 1 1 3.0 Clc1ccc2c(c1Cl)CNCCC2 10.1021/jm0205752
CHEMBL38681 148673 20 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibitory potency against alpha-2-adrenoceptorInhibitory potency against alpha-2-adrenoceptor
ChEMBL 215 0 1 1 3.0 Clc1ccc2c(c1Cl)CNCCC2 10.1021/jm0205752
10436842 107032 0 None -5754 7 Human 5.3 pKi = 5.3 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL288772 107032 0 None -5754 7 Human 5.3 pKi = 5.3 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
57326586 80841 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 402 5 1 7 2.5 OCCOCCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL2022275 80841 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 402 5 1 7 2.5 OCCOCCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
44438165 173563 0 None -48 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 467 9 1 7 3.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCCN(C)C)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL428407 173563 0 None -48 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 467 9 1 7 3.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCCN(C)C)cc13)CC2 10.1016/j.bmcl.2006.12.094
16007117 86811 0 None -457 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 86811 0 None -457 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415704 86934 0 None -158 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 86934 0 None -158 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
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
155538007 179134 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 444 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4475933 179134 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 444 7 0 6 4.1 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
3561 25849 39 None -1 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 25849 39 None -1 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
499 10849 18 None -346 14 Rat 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
5685 10849 18 None -346 14 Rat 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
CHEMBL25554 10849 18 None -346 14 Rat 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm00018a001
11300487 91777 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
CHEMBL223830 91777 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1ccccc1-c1ccccc1OC(C)C1=NCCN1 10.1021/jm0408215
10467319 210621 14 None -9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at alpha-2 adrenergic receptor of rat.Binding affinity at alpha-2 adrenergic receptor of rat.
ChEMBL 250 0 2 1 2.6 Brc1cccc2c3c([nH]c12)CNCC3 10.1016/j.bmcl.2003.11.078
CHEMBL6857 210621 14 None -9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at alpha-2 adrenergic receptor of rat.Binding affinity at alpha-2 adrenergic receptor of rat.
ChEMBL 250 0 2 1 2.6 Brc1cccc2c3c([nH]c12)CNCC3 10.1016/j.bmcl.2003.11.078
6455104 105262 6 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 172 2 1 2 1.7 C(=C/c1ccccc1)\C1=NCCN1 10.1021/acs.jmedchem.9b02080
CHEMBL275970 105262 6 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 172 2 1 2 1.7 C(=C/c1ccccc1)\C1=NCCN1 10.1021/acs.jmedchem.9b02080
15853467 214913 0 None -141 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2A adrenergic receptorBinding affinity against human Alpha-2A adrenergic receptor
ChEMBL 692 16 3 8 5.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN=[N+]=[N-])N1 10.1016/s0960-894x(99)00484-9
CHEMBL98063 214913 0 None -141 6 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Alpha-2A adrenergic receptorBinding affinity against human Alpha-2A adrenergic receptor
ChEMBL 692 16 3 8 5.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCN=[N+]=[N-])N1 10.1016/s0960-894x(99)00484-9
44574134 185283 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466634 185283 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44387798 173052 0 None -4 2 Human 7.3 pKi = 7.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 458 7 0 5 3.9 CC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(CCC/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
CHEMBL426959 173052 0 None -4 2 Human 7.3 pKi = 7.3 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 458 7 0 5 3.9 CC(=O)N1C[C@@H]2C(=NO[C@H]2CN2CCN(CCC/C=C/c3ccccc3)CC2)c2ccccc21 10.1021/jm049619s
11108001 17644 2 None -4 6 Human 7.3 pKi = 7.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 17644 2 None -4 6 Human 7.3 pKi = 7.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 17644 2 None -4 6 Human 7.3 pKi = 7.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
44352207 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
CHEMBL128168 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm800250z
44352207 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL128168 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
44352207 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL128168 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
44352207 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL128168 25628 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 CC(Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
162674829 190053 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 513 11 5 11 1.2 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4796664 190053 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 513 11 5 11 1.2 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
164614469 191560 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 341 1 0 3 3.9 C[Si](C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4851349 191560 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 341 1 0 3 3.9 C[Si](C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
13149 9323 36 None -77 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.9b01465
3034396 9323 36 None -77 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.9b01465
CHEMBL299031 9323 36 None -77 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 minsDisplacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.9b01465
44269013 37115 1 None 1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL13917 37115 1 None 1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 218 5 1 3 2.0 CCCc1ccccc1OCC1=NCCN1 10.1021/ml400232p
45487962 204264 0 None 10 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 218 4 1 3 2.1 CCCc1ccccc1COC1=NCCN1 10.1021/jm901262f
CHEMBL569933 204264 0 None 10 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 218 4 1 3 2.1 CCCc1ccccc1COC1=NCCN1 10.1021/jm901262f
11776640 20318 0 None 2 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1193824 20318 0 None 2 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL545293 20318 0 None 2 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
163198500 193177 3 None -3 2 Human 5.3 pKi = 5.3 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
CHEMBL4875858 193177 3 None -3 2 Human 5.3 pKi = 5.3 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
15407445 207057 2 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 192 1 1 3 1.6 CC1Cc2ccc([N+](=O)[O-])cc2CN1 10.1016/j.bmcl.2004.12.013
CHEMBL59719 207057 2 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 192 1 1 3 1.6 CC1Cc2ccc([N+](=O)[O-])cc2CN1 10.1016/j.bmcl.2004.12.013
132060743 169015 0 None -1 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 169015 0 None -1 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK 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
57395732 77966 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 342 5 1 3 4.8 CC(Oc1c(-c2ccccc2)cccc1-c1ccccc1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956203 77966 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 342 5 1 3 4.8 CC(Oc1c(-c2ccccc2)cccc1-c1ccccc1)C1=NCCN1 10.1016/j.bmc.2012.01.035
70696790 83074 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 194 3 1 3 1.5 CC1COC(NC(C2CC2)C2CC2)=N1 10.1016/j.bmc.2012.06.008
CHEMBL2058632 83074 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 194 3 1 3 1.5 CC1COC(NC(C2CC2)C2CC2)=N1 10.1016/j.bmc.2012.06.008
90644748 119512 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 4 4 2 3.6 CCNc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289520 119512 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 4 4 2 3.6 CCNc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304855 119512 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 254 4 4 2 3.6 CCNc1ccc(NC(=N)Nc2ccccc2)cc1 10.1016/j.ejmech.2014.05.057
155517797 176992 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 498 8 0 6 5.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CC34CC5CC(CC(C5)C3)C4)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4445396 176992 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 498 8 0 6 5.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(CC34CC5CC(CC(C5)C3)C4)C(=O)C21 10.1021/acs.jmedchem.9b02080
102 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
3659 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
8969 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
CHEMBL15245 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
DB01392 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
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 10.1021/jm00366a007
102 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
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 10.1021/jm00150a002
3659 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
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 10.1021/jm00150a002
8969 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
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 10.1021/jm00150a002
CHEMBL15245 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
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 10.1021/jm00150a002
DB01392 10899 48 None -47 49 Bovine 7.3 pKi = 7.3 Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortexEvaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
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 10.1021/jm00150a002
191 7191 98 None -41 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 7191 98 None -41 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 7191 98 None -41 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 7191 98 None -41 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 7191 98 None -41 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
13298530 105848 20 None 97 2 Bovine 8.3 pKi = 8.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00366a007
CHEMBL280514 105848 20 None 97 2 Bovine 8.3 pKi = 8.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 195 1 0 3 1.0 CN1CCN(c2ncccc2F)CC1 10.1021/jm00366a007
44215744 214221 0 None -1 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccc5ccccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL94129 214221 0 None -1 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4ccc5ccccc5c4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
521 8186 69 None -2 7 Rat 8.3 pKi = 8.3 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
5311068 8186 69 None -2 7 Rat 8.3 pKi = 8.3 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
835 8186 69 None -2 7 Rat 8.3 pKi = 8.3 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
CHEMBL778 8186 69 None -2 7 Rat 8.3 pKi = 8.3 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
DB00633 8186 69 None -2 7 Rat 8.3 pKi = 8.3 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 10.1021/jm000128r
42267840 22376 2 None 4 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 425 7 1 5 2.9 COc1ccccc1N1CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221499 22376 2 None 4 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 425 7 1 5 2.9 COc1ccccc1N1CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
44330857 11166 0 None -5 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 493 8 0 8 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4OC)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL101361 11166 0 None -5 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 493 8 0 8 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4OC)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
294234 109670 3 None 1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
CHEMBL305928 109670 3 None 1 4 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 182 1 1 3 1.7 C1CCCC(NC2=NCCO2)CC1 10.1016/0960-894X(94)85032-1
31101 7516 40 None -10 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 7516 40 None -10 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 7516 40 None -10 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 7516 40 None -10 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 7516 40 None -10 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
13123525 195977 0 None - 1 Bovine 8.3 pKi = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 265 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)c2ccccc2)cc1 10.1021/jm00366a022
CHEMBL51131 195977 0 None - 1 Bovine 8.3 pKi = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 265 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)c2ccccc2)cc1 10.1021/jm00366a022
44330598 214417 0 None -8 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4cccc(F)c4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL95218 214417 0 None -8 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4cccc(F)c4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
10220053 213699 0 None 3 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1016/s0960-894x(03)00525-0
CHEMBL90997 213699 0 None 3 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1016/s0960-894x(03)00525-0
10220053 213699 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1021/jm049619s
CHEMBL90997 213699 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptorInhibition of [3H]- rauwolscine binding to human alpha-2A adrenergic receptor
ChEMBL 218 2 1 2 1.9 Fc1ccc2c(c1)CC(CC1CN=CN1)C2 10.1021/jm049619s
1343 8670 62 None -11 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 8670 62 None -11 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 8670 62 None -11 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 8670 62 None -11 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 8670 62 None -11 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
100 10577 58 None -33 54 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -33 54 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -33 54 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -33 54 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -33 54 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
73291731 99266 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL2431282 99266 0 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 232 5 1 3 2.4 CCCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
117590588 103299 35 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O 10.1021/jm001040g
14969 103299 35 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O 10.1021/jm001040g
CHEMBL262777 103299 35 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O 10.1021/jm001040g
24906199 194444 15 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL495096 194444 15 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 258 4 1 3 3.1 CC(Oc1ccccc1C1CCCC1)C1=NCCN1 10.1021/jm800250z
45487955 205089 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 232 4 1 3 2.7 CCCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL576078 205089 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 232 4 1 3 2.7 CCCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
2771431 195061 52 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 231 1 1 3 1.8 Clc1cnc(N2CCNCC2)c(Cl)c1 10.1021/jm00366a007
CHEMBL50016 195061 52 None 1 2 Bovine 6.3 pKi = 6.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 231 1 1 3 1.8 Clc1cnc(N2CCNCC2)c(Cl)c1 10.1021/jm00366a007
9923679 88537 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1021/jm060262x
CHEMBL216399 88537 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 332 3 1 4 4.0 Cc1cc(Nc2ccc(N3CCN(C)CC3)cc2)c2ccccc2n1 10.1021/jm060262x
162651072 186959 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 527 12 5 11 1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4749263 186959 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 527 12 5 11 1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
137641762 164878 0 None -15 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptorDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor
ChEMBL 476 5 4 10 1.1 CCCNc1nc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.7b00141
CHEMBL4086593 164878 0 None -15 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptorDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor
ChEMBL 476 5 4 10 1.1 CCCNc1nc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.7b00141
137643541 165210 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptorDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor
ChEMBL 448 3 4 10 0.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00141
CHEMBL4090355 165210 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptorDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor
ChEMBL 448 3 4 10 0.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00141
3158 63041 27 None -3467 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 63041 27 None -3467 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10651080 112719 0 None -57 6 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL312871 112719 0 None -57 6 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 592 9 3 6 4.7 CC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
57398332 78022 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc(C2COC(C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956900 78022 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc(C2COC(C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
10916464 210932 0 None -10 5 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70563 210932 0 None -10 5 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
44579184 197732 4 None -10 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 340 4 0 5 2.7 COc1ccccc1N1CCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL518592 197732 4 None -10 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 340 4 0 5 2.7 COc1ccccc1N1CCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
132060776 169181 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 169181 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
11820657 20216 1 None 6 2 Bovine 7.3 pKi = 7.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
CHEMBL1193017 20216 1 None 6 2 Bovine 7.3 pKi = 7.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
CHEMBL544354 20216 1 None 6 2 Bovine 7.3 pKi = 7.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
10036255 28131 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1cccc2c1CC1(CC2)CN=CN1 10.1021/jm00020a021
CHEMBL131417 28131 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1cccc2c1CC1(CC2)CN=CN1 10.1021/jm00020a021
10036256 30553 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1ccc2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
CHEMBL133579 30553 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1ccc2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
11277479 91525 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
CHEMBL222973 91525 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 4 1 3 3.4 Cc1cccc(-c2ccccc2OC(C)C2=NCCN2)c1 10.1021/jm0408215
10214826 11251 20 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 289 2 2 4 2.9 Brc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
CHEMBL1019 11251 20 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 289 2 2 4 2.9 Brc1c(Nc2ncc[nH]2)ccc2nccnc12 10.1021/jm9605142
130442572 178687 0 None -109 24 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -109 24 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK 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
90644706 119520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 269 3 3 2 3.3 N=C(NCc1ccco1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3289531 119520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 269 3 3 2 3.3 N=C(NCc1ccco1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3304994 119520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 269 3 3 2 3.3 N=C(NCc1ccco1)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
4735 201894 96 None -9 10 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL361506 201894 96 None -9 10 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
CHEMBL55 201894 96 None -9 10 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 nan
3584 10549 64 None -251 14 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
5401 10549 64 None -251 14 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
7302 10549 64 None -251 14 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
CHEMBL611 10549 64 None -251 14 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
DB01162 10549 64 None -251 14 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 nan
10101373 19865 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 718 6 6 6 4.6 O=C(NCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL1190317 19865 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 718 6 6 6 4.6 O=C(NCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
CHEMBL540594 19865 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
ChEMBL 718 6 6 6 4.6 O=C(NCCCNC(=O)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21)[C@H]1[C@@H](O)CC[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@@H]21 10.1016/s0960-894x(00)00068-8
24882007 19245 1 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.ejmech.2014.09.083
CHEMBL1186220 19245 1 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 201 1 2 3 0.3 c1ccc2c(c1)cnn2N=C1NCCN1 10.1016/j.ejmech.2014.09.083
49836301 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
CHEMBL1276140 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml400232p
49836301 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
CHEMBL1276140 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/jm100977d
49836301 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml300064v
CHEMBL1276140 25339 1 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1O[C@@H](C)C1=NCCN1 10.1021/ml300064v
16785637 188356 80 None 11 2 Bovine 5.3 pKi = 5.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 206 2 2 4 -0.4 NC(=O)c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL47688 188356 80 None 11 2 Bovine 5.3 pKi = 5.3 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 206 2 2 4 -0.4 NC(=O)c1cccnc1N1CCNCC1 10.1021/jm00366a007
162664704 188990 0 None - 1 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 471 8 5 11 0.2 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2CNCc3ccccc32)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4783068 188990 0 None - 1 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 471 8 5 11 0.2 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2CNCc3ccccc32)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
73347825 99315 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432046 99315 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
145973771 171498 0 None -6 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 171498 0 None -6 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]Rauwolscine from human adrenergic alpha2A receptor expressed in MDCK cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
448537 167029 89 None -33 25 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 167029 89 None -33 25 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
155521287 177357 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4450506 177357 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
487 10406 21 None -1513 12 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
60602 10406 21 None -1513 12 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
CHEMBL405355 10406 21 None -1513 12 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
DB09239 10406 21 None -1513 12 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
10059780 19731 0 None 6 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1189347 19731 0 None 6 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL538537 19731 0 None 6 3 Bovine 6.3 pKi = 6.3 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
289 7030 12 None -47 14 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha2A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 7030 12 None -47 14 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha2A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 7030 12 None -47 14 Human 6.3 pKi = 6.3 Binding
Binding affinity to human adrenergic alpha2A receptor by radioligand displacement assayBinding affinity to human adrenergic alpha2A receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
2398 7741 62 None -14 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 7741 62 None -14 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 7741 62 None -14 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 7741 62 None -14 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 7741 62 None -14 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
162643475 188522 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha 2A adrenoceptor (unknown origin)Binding affinity to alpha 2A adrenoceptor (unknown origin)
ChEMBL 283 1 0 2 4.3 C=C1CCN2Cc3ccc(OC)cc3[C@H]3CCCC[C@]32C1 10.1021/acs.jmedchem.0c01192
CHEMBL4777306 188522 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to alpha 2A adrenoceptor (unknown origin)Binding affinity to alpha 2A adrenoceptor (unknown origin)
ChEMBL 283 1 0 2 4.3 C=C1CCN2Cc3ccc(OC)cc3[C@H]3CCCC[C@]32C1 10.1021/acs.jmedchem.0c01192
15730 77893 80 None -2 10 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 77893 80 None -2 10 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
155521287 177357 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4450506 177357 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
57394788 78025 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@H]2COC[C@@H](C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956903 78025 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@H]2COC[C@@H](C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
10092819 23545 0 None -51 11 Rat 7.3 pKi = 7.3 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
CHEMBL124444 23545 0 None -51 11 Rat 7.3 pKi = 7.3 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
44424855 92229 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
CHEMBL226636 92229 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
518 10384 1 None -3 6 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
9839317 10384 1 None -3 6 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
CHEMBL123138 10384 1 None -3 6 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 299 0 0 2 3.8 CN1CCc2c3c(C1)c(Br)oc3ccc2Cl 10.1021/jm00019a001
49781005 23986 0 None 3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
CHEMBL1256503 23986 0 None 3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 226 2 1 2 2.5 CO[C@H]1c2ccccc2[C@H]2C[C@@]12c1c[nH]cn1 10.1021/jm1006269
6075 156887 42 None -11 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 156887 42 None -11 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
155548049 180476 0 None -3 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 266 1 2 3 3.3 O=C1/C(=C/c2cccc(O)c2)CCc2c(O)cccc21 10.1016/j.ejmech.2021.113964
CHEMBL4535634 180476 0 None -3 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 266 1 2 3 3.3 O=C1/C(=C/c2cccc(O)c2)CCc2c(O)cccc21 10.1016/j.ejmech.2021.113964
135559170 108837 0 None -851 7 Human 6.3 pKi = 6.3 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
CHEMBL302021 108837 0 None -851 7 Human 6.3 pKi = 6.3 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
3584 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
5401 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
7302 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
CHEMBL611 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
DB01162 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm980077m
9813756 15788 0 None -1 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL109848 15788 0 None -1 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
13123534 196232 1 None - 1 Bovine 7.3 pKi = 7.3 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/jm00366a022
CHEMBL51358 196232 1 None - 1 Bovine 7.3 pKi = 7.3 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
ChEMBL 209 3 2 3 1.8 Clc1ccccc1NCC1=NCCN1 10.1021/jm00366a022
2142 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
4920903 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
502 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
5775 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
CHEMBL597 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
DB00692 9870 58 None -2 37 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1016/j.bmcl.2005.07.083
3584 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
5401 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
7302 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
CHEMBL611 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
DB01162 10549 64 None -251 14 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1021/jm00010a001
12613159 194105 11 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL493054 194105 11 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
11465618 109175 23 None -2089 19 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 109175 23 None -2089 19 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 109175 23 None -2089 19 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]RX 821002 from recombinant human alpha2A receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]RX 821002 from recombinant human alpha2A 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
9816461 17491 7 None -9 4 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 17491 7 None -9 4 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 17491 7 None -9 4 Human 5.3 pKi = 5.3 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
24906198 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
CHEMBL495095 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml400232p
57402717 77962 2 None 14 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956199 77962 2 None 14 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 220 4 1 4 1.5 COc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
24906198 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL495095 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
45487145 204438 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 230 4 1 3 2.5 C=CCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
CHEMBL570973 204438 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 230 4 1 3 2.5 C=CCc1ccccc1C(C)OC1=NCCN1 10.1021/jm901262f
24906198 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
CHEMBL495095 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/jm100977d
24906198 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml300064v
CHEMBL495095 194443 3 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 230 5 1 3 2.2 C=CCc1ccccc1OC(C)C1=NCCN1 10.1021/ml300064v
44329027 10940 0 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 637 13 3 7 4.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL100045 10940 0 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 637 13 3 7 4.9 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COC)N1 10.1016/s0960-894x(99)00484-9
11097789 109775 1 None -11 6 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 109775 1 None -11 6 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
2765 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
515 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
CHEMBL13852 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
DB09202 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/ml400232p
2765 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
515 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
CHEMBL13852 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
DB09202 7730 19 None -1 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1021/jm901262f
16090621 148353 0 None -16 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1021/jm060262x
CHEMBL384925 148353 0 None -16 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 422 5 1 4 5.6 Cc1nc2ccccc2c(Nc2ccc(N3CCN(C)CC3)cc2)c1Cc1ccccc1 10.1021/jm060262x
1960 9632 67 None -35 26 Mouse 5.2 pKi = 5.2 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
439260 9632 67 None -35 26 Mouse 5.2 pKi = 5.2 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
505 9632 67 None -35 26 Mouse 5.2 pKi = 5.2 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL1437 9632 67 None -35 26 Mouse 5.2 pKi = 5.2 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
DB00368 9632 67 None -35 26 Mouse 5.2 pKi = 5.2 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O nan
9906978 49485 2 None -165 12 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 49485 2 None -165 12 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assayBinding affinity to human cloned adrenergic alpha-2A receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
6726 8063 51 None -10 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 8063 51 None -10 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 8063 51 None -10 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 8063 51 None -10 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 8063 51 None -10 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
150 9287 21 None -45 16 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 9287 21 None -45 16 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 9287 21 None -45 16 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 9287 21 None -45 16 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 9287 21 None -45 16 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
9859437 174801 0 None 38 3 Human 8.2 pKi = 8.2 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
CHEMBL432155 174801 0 None 38 3 Human 8.2 pKi = 8.2 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 230 2 3 4 2.3 Cc1c(Nc2ncc[nH]2)ccc2c1NCCO2 10.1021/jm9605142
49864360 22399 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 445 10 1 4 5.0 COc1ccccc1N1CCN(CCCCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221593 22399 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 445 10 1 4 5.0 COc1ccccc1N1CCN(CCCCCCNC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
11653915 130790 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 296 4 2 5 2.6 COc1cccc(N(NC2=NCCN2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
CHEMBL362954 130790 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cellsBinding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
ChEMBL 296 4 2 5 2.6 COc1cccc(N(NC2=NCCN2)c2ccc(C)cc2)c1 10.1016/j.bmcl.2005.07.083
1209 8439 75 None -1 32 Human 8.2 pKi = 8.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1021/jm001040g
203 8439 75 None -1 32 Human 8.2 pKi = 8.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1021/jm001040g
3386 8439 75 None -1 32 Human 8.2 pKi = 8.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1021/jm001040g
CHEMBL41 8439 75 None -1 32 Human 8.2 pKi = 8.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1021/jm001040g
DB00472 8439 75 None -1 32 Human 8.2 pKi = 8.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1021/jm001040g
131829 211506 15 None 7 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
CHEMBL74283 211506 15 None 7 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 295 1 4 5 1.7 Brc1c(NC2=NCCN2)ccc2c1NCCN2 10.1016/0960-894X(95)00391-6
135477797 85707 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112971 85707 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
2435 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
395 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
520 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
5386 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
CHEMBL844 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
DB00484 7509 100 None -2 12 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1016/0960-894X(95)00391-6
10382537 210945 12 None 6 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL70676 210945 12 None 6 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 339 1 2 5 1.6 Ic1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
98358 126264 8 None -1 2 Bovine 7.2 pKi = 7.2 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL345349 126264 8 None -1 2 Bovine 7.2 pKi = 7.2 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
98358 126264 8 None -1 2 Bovine 7.2 pKi = 7.2 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
CHEMBL345349 126264 8 None -1 2 Bovine 7.2 pKi = 7.2 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 226 0 1 1 3.3 c1ccc2c3c([nH]c2c1)C1CCCCN1CC3 10.1021/jm00398a025
11361608 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL222928 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
11361608 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
CHEMBL222928 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm0408215
11361608 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL222928 91520 1 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 CC(Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
13141186 137469 0 None -7 2 Bovine 6.2 pKi = 6.2 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 312 0 0 2 4.2 CN1CCC(=C2c3cc(Cl)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368357 137469 0 None -7 2 Bovine 6.2 pKi = 6.2 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 312 0 0 2 4.2 CN1CCC(=C2c3cc(Cl)ccc3CCn3cccc32)CC1 10.1021/jm00361a008
9851486 213478 0 None -512 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL89685 213478 0 None -512 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 592 10 2 6 6.0 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
155525779 177821 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 494 7 0 6 5.3 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3cc(Cl)cc(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4456882 177821 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 494 7 0 6 5.3 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3cc(Cl)cc(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
11771731 115023 2 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL319706 115023 2 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)Displacement of [3H]RX821002 from alpha-2A adrenergic receptor (unknown origin)
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
134 9292 24 None -74 67 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 9292 24 None -74 67 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 9292 24 None -74 67 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 9292 24 None -74 67 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 9292 24 None -74 67 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
489 6933 28 None -1778 12 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
5640 6933 28 None -1778 12 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
CHEMBL420060 6933 28 None -1778 12 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
ChEMBL 401 7 1 8 1.0 COc1ccccc1N1CCN(CC1)CCCNc1c(C)c(=O)n(c(=O)n1C)C 10.1021/jm00018a001
10082625 20565 0 None -4 3 Bovine 6.2 pKi = 6.2 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1195526 20565 0 None -4 3 Bovine 6.2 pKi = 6.2 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL554785 20565 0 None -4 3 Bovine 6.2 pKi = 6.2 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
2750 210840 76 None -3 12 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 210840 76 None -3 12 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
2351 10059 64 None -9 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -9 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -9 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -9 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -9 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
129211 10521 78 None -120 16 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligandBinding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
2562 10521 78 None -120 16 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligandBinding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
488 10521 78 None -120 16 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligandBinding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
CHEMBL836 10521 78 None -120 16 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligandBinding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
DB00706 10521 78 None -120 16 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligandBinding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm9905918
2274 9947 58 None -10 31 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -10 31 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -10 31 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -10 31 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -10 31 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10934575 211265 0 None -3 6 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 211265 0 None -3 6 Human 7.2 pKi = 7.2 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
10823140 127144 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 2 1 2 2.5 C1=NC[C@H](C[C@]23CCc4ccccc4C2C3)N1 10.1021/jm001040g
136078488 127144 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 2 1 2 2.5 C1=NC[C@H](C[C@]23CCc4ccccc4C2C3)N1 10.1021/jm001040g
CHEMBL353212 127144 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cellBinding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
ChEMBL 226 2 1 2 2.5 C1=NC[C@H](C[C@]23CCc4ccccc4C2C3)N1 10.1021/jm001040g
75306277 116031 0 None -31 23 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 116031 0 None -31 23 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assayBinding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
155550341 181882 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 458 8 0 6 4.2 CCOP(=O)(OCC)C1(Cc2ccc(F)cc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4568994 181882 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 458 8 0 6 4.2 CCOP(=O)(OCC)C1(Cc2ccc(F)cc2)N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
1042 8362 23 None -97 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 8362 23 None -97 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 8362 23 None -97 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 8362 23 None -97 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 8362 23 None -97 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
16090635 89290 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 378 4 1 4 4.7 CCc1c(C)nc2c(c1Nc1ccc(N3CCN(C)C(C)C3)cc1)CCCC2 10.1021/jm060262x
CHEMBL217768 89290 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 378 4 1 4 4.7 CCc1c(C)nc2c(c1Nc1ccc(N3CCN(C)C(C)C3)cc1)CCCC2 10.1021/jm060262x
10508332 112768 0 None -426 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 638 11 2 8 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1021/jm980077m
CHEMBL313160 112768 0 None -426 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 638 11 2 8 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])c(OC)c1 10.1021/jm980077m
10626982 118272 0 None -11 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
CHEMBL327775 118272 0 None -11 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 575 9 2 6 5.9 CC1=C(C#N)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C)N1 10.1021/jm980077m
1534 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
155536080 178893 0 None -43 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 178893 0 None -43 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human recombinant adrenergic Alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
57394789 78026 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@@H]2COC[C@@H](C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956904 78026 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@@H]2COC[C@@H](C3=NCCN3)O2)cc1 10.1016/j.bmc.2012.02.016
1534 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 109817 53 None -6 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Clonidine from human recombinant adrenergic alpha2A receptor expressed in MDCK cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
162677211 190339 0 None - 1 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 516 9 5 13 -0.0 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccc([N+](=O)[O-])cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4800292 190339 0 None - 1 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 516 9 5 13 -0.0 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCNCC2Cc3ccc([N+](=O)[O-])cc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
487 10406 21 None -1513 12 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
60602 10406 21 None -1513 12 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
CHEMBL405355 10406 21 None -1513 12 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
DB09239 10406 21 None -1513 12 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00019a001
10793963 106448 0 None -69 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL284470 106448 0 None -69 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 622 11 2 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
71652196 94229 0 None -190 6 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL2333732 94229 0 None -190 6 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
3652 53018 70 None -1 9 Human 5.2 pKi = 5.2 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
CHEMBL1535 53018 70 None -1 9 Human 5.2 pKi = 5.2 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
118717249 121903 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 219 1 2 3 0.5 Fc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.ejmech.2014.09.083
CHEMBL3343700 121903 0 None 2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation countingDisplacement of [3H]RS-79948-197 from human alpha2A adrenoceptor expressed in CHO-K1 cells after 45 mins by liquid scintillation counting
ChEMBL 219 1 2 3 0.5 Fc1cccc2cnn(N=C3NCCN3)c12 10.1016/j.ejmech.2014.09.083
11741010 90026 0 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1cc(C)c2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
CHEMBL218730 90026 0 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1cc(C)c2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
164609539 191178 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4845850 191178 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
123920 106930 41 None -309 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 201 0 1 1 2.6 Clc1ccc2c(c1Cl)CNCC2 10.1016/j.bmcl.2004.12.013
CHEMBL287837 106930 41 None -309 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligandBinding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand
ChEMBL 201 0 1 1 2.6 Clc1ccc2c(c1Cl)CNCC2 10.1016/j.bmcl.2004.12.013
71459553 90471 10 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
CHEMBL2205360 90471 10 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
1960 9632 67 None -23 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
439260 9632 67 None -23 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
505 9632 67 None -23 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
CHEMBL1437 9632 67 None -23 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
DB00368 9632 67 None -23 26 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960012o
44325044 214162 0 None -5 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 479 6 0 8 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4csc5ccccc45)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL93801 214162 0 None -5 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 479 6 0 8 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4csc5ccccc45)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
44401164 76591 0 None -346 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 76591 0 None -346 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
44579271 193873 0 None -32 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 475 9 0 7 4.2 c1ccc(Oc2ncccc2COCCN2CCCN(CC3COc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
CHEMBL491419 193873 0 None -32 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 475 9 0 7 4.2 c1ccc(Oc2ncccc2COCCN2CCCN(CC3COc4ccccc4O3)CC2)cc1 10.1016/j.bmcl.2008.08.055
14004035 126297 0 None -1 2 Bovine 6.2 pKi = 6.2 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
CHEMBL345621 126297 0 None -1 2 Bovine 6.2 pKi = 6.2 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
14004035 126297 0 None -1 2 Bovine 6.2 pKi = 6.2 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
CHEMBL345621 126297 0 None -1 2 Bovine 6.2 pKi = 6.2 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 227 0 1 2 2.6 c1cnc2[nH]c3c(c2c1)CCN1CCCCC31 10.1021/jm00398a025
24906160 176235 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
CHEMBL442815 176235 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 247 5 1 5 1.4 CO/N=C/c1ccccc1OC(C)C1=NCCN1 10.1021/jm800250z
441082 7946 48 None -141 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
8981 7946 48 None -141 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
CHEMBL191703 7946 48 None -141 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cellsDisplacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
122442272 145126 0 None -11 15 Human 6.2 pKi = 6.2 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 145126 0 None -11 15 Human 6.2 pKi = 6.2 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 145126 0 None -11 15 Human 6.2 pKi = 6.2 Binding
Binding affinity to human alpha-2A adrenergic receptor by radioligand binding assayBinding affinity to human alpha-2A adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
240 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 7731 43 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
196129 74573 17 None -85 15 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 74573 17 None -85 15 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
26757 214757 31 None -1 2 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 nan
CHEMBL972 214757 31 None -1 2 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 nan
10818003 113198 0 None -12 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1021/jm980077m
CHEMBL313953 113198 0 None -12 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 649 12 3 6 6.2 CC(C)C1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(C(C)C)N1 10.1021/jm980077m
10603951 213295 0 None -33 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 622 10 1 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
CHEMBL88448 213295 0 None -33 6 Human 6.2 pKi = 6.2 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 622 10 1 7 6.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)N(C)CCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980077m
90644753 119545 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 231 3 3 1 2.9 CCCNC(=N)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3289537 119545 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 231 3 3 1 2.9 CCCNC(=N)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
CHEMBL3305462 119545 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 231 3 3 1 2.9 CCCNC(=N)Nc1ccc2c(c1)CCCC2 10.1016/j.ejmech.2014.05.057
3073596 51021 28 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 184 1 1 2 2.8 c1ccc2oc(-c3ncc[nH]3)cc2c1 10.1021/acs.jmedchem.9b02080
CHEMBL151697 51021 28 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 184 1 1 2 2.8 c1ccc2oc(-c3ncc[nH]3)cc2c1 10.1021/acs.jmedchem.9b02080
9816063 109851 0 None -4 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
CHEMBL30739 109851 0 None -4 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm990569e
9816063 109851 0 None 4 6 Rat 7.2 pKi = 7.2 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm000128r
CHEMBL30739 109851 0 None 4 6 Rat 7.2 pKi = 7.2 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 232 1 1 2 3.6 Cc1sc(C)c2c1CCCC2c1c[nH]cn1 10.1021/jm000128r
16090625 89205 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1nc2cccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL217452 89205 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1nc2cccc(C)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
130442480 182049 0 None -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-rauwolscine from recombinant human alpha2A adrenergic receptor stably expressed in MDCK 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
155556618 181256 0 None -6456 5 Human 5.2 pKi = 5.2 Binding
Inhibition of alpha2a receptor (unknown origin)Inhibition of alpha2a receptor (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4554295 181256 0 None -6456 5 Human 5.2 pKi = 5.2 Binding
Inhibition of alpha2a receptor (unknown origin)Inhibition of alpha2a receptor (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
4011 89183 49 None -35 24 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 89183 49 None -35 24 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
28417 46813 49 None -1 12 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 46813 49 None -1 12 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
26987 7736 33 None -158 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 7736 33 None -158 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 7736 33 None -158 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 7736 33 None -158 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 7736 33 None -158 21 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
16215415 194111 1 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]MK912 from human cloned adrenergic alpha-2a receptorDisplacement of [3H]MK912 from human cloned adrenergic alpha-2a receptor
ChEMBL 471 9 2 3 3.8 CN(C)CCCOc1ccc(CCNC(=O)c2cc(Br)c[nH]2)cc1Br 10.1021/np800339e
CHEMBL493091 194111 1 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]MK912 from human cloned adrenergic alpha-2a receptorDisplacement of [3H]MK912 from human cloned adrenergic alpha-2a receptor
ChEMBL 471 9 2 3 3.8 CN(C)CCCOc1ccc(CCNC(=O)c2cc(Br)c[nH]2)cc1Br 10.1021/np800339e
44330621 11174 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 483 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccc(Cl)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL101411 11174 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 483 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccc(Cl)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
90644738 119510 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 281 2 2 2 3.1 c1coc(C2CN/C(=N/c3ccc4c(c3)CCCC4)N2)c1 10.1016/j.ejmech.2014.05.057
CHEMBL3289548 119510 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 281 2 2 2 3.1 c1coc(C2CN/C(=N/c3ccc4c(c3)CCCC4)N2)c1 10.1016/j.ejmech.2014.05.057
CHEMBL3304843 119510 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 281 2 2 2 3.1 c1coc(C2CN/C(=N/c3ccc4c(c3)CCCC4)N2)c1 10.1016/j.ejmech.2014.05.057
155526672 177988 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 528 7 0 6 6.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3c(Cl)cc(Cl)cc3Cl)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4459403 177988 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 528 7 0 6 6.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3c(Cl)cc(Cl)cc3Cl)C(=O)C21 10.1021/acs.jmedchem.9b02080
155535203 178820 0 None -18 6 Human 5.2 pKi = 5.2 Binding
Inhibition of alpha2a receptor (unknown origin)Inhibition of alpha2a receptor (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL4471712 178820 0 None -18 6 Human 5.2 pKi = 5.2 Binding
Inhibition of alpha2a receptor (unknown origin)Inhibition of alpha2a receptor (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
10198108 214984 2 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 200 0 1 2 1.9 Cc1ccc2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
CHEMBL98471 214984 2 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 200 0 1 2 1.9 Cc1ccc2c(c1)CC1(CC2)CN=CN1 10.1021/jm00020a021
12575 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
54459 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
CHEMBL10316 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1021/jm800250z
12575 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmc.2012.02.016
54459 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmc.2012.02.016
CHEMBL10316 8769 30 None -5 17 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmc.2012.02.016
12774559 196388 0 None - 1 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 191 3 3 4 0.8 Oc1cccc(NCC2=NCCN2)c1 10.1021/jm00366a022
CHEMBL51479 196388 0 None - 1 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 191 3 3 4 0.8 Oc1cccc(NCC2=NCCN2)c1 10.1021/jm00366a022
185076 193869 5 None 2 7 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
CHEMBL49137 193869 5 None 2 7 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 227 1 2 5 1.3 Cc1c(NC2=NCCN2)ccc2nccnc12 10.1016/0960-894X(95)00391-6
213041 23905 28 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 230 2 1 1 3.0 CCC1(c2c[nH]cn2)Cc2ccc(F)cc2C1 10.1021/jm1006269
CHEMBL1255582 23905 28 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
ChEMBL 230 2 1 1 3.0 CCC1(c2c[nH]cn2)Cc2ccc(F)cc2C1 10.1021/jm1006269
102 10899 48 None -5 49 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
3659 10899 48 None -5 49 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
8969 10899 48 None -5 49 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
CHEMBL15245 10899 48 None -5 49 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
DB01392 10899 48 None -5 49 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
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 10.1021/jm00019a001
155513073 176494 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 440 8 0 6 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(Cc3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4438158 176494 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 440 8 0 6 4.0 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(Cc3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
11412944 108286 69 None 223 2 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL298004 108286 69 None 223 2 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 197 1 1 3 1.1 Clc1cccnc1N1CCNCC1 10.1021/jm00366a007
135545454 85718 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 448 7 1 7 3.2 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112983 85718 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 448 7 1 7 3.2 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CN2 10.1021/jm049619s
2803 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
516 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
704 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
CHEMBL134 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
DB00575 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscineBinding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/0960-894X(94)85032-1
13123533 201688 1 None - 1 Bovine 7.2 pKi = 7.2 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 271 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)C2CCCCC2)cc1 10.1021/jm00366a022
CHEMBL541208 201688 1 None - 1 Bovine 7.2 pKi = 7.2 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 271 4 1 3 3.1 Cc1ccc(N(CC2=NCCN2)C2CCCCC2)cc1 10.1021/jm00366a022
155544935 180196 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 460 7 0 6 4.6 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccccc3Cl)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4528557 180196 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 460 7 0 6 4.6 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccccc3Cl)C(=O)C21 10.1021/acs.jmedchem.9b02080
162654541 187392 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 499 10 5 11 0.8 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
CHEMBL4754656 187392 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assayDisplacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay
ChEMBL 499 10 5 11 0.8 Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCCCCNCC2Cc3ccccc3CN2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.0c01475
10045713 172884 0 None -309 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1021/jm060262x
CHEMBL425983 172884 0 None -309 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 386 3 1 4 5.3 Cc1nc2ccccc2c(Nc2ccc(N3CCN4CCCCC4C3)cc2)c1C 10.1021/jm060262x
122186880 129758 0 None -7 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha2A adrenoceptor (unknown origin)Binding affinity to alpha2A adrenoceptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 129758 0 None -7 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha2A adrenoceptor (unknown origin)Binding affinity to alpha2A adrenoceptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44401106 131105 0 None -112 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL363581 131105 0 None -112 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
57345627 77957 0 None 8 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 230 4 1 3 2.5 C=C(C)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956194 77957 0 None 8 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 230 4 1 3 2.5 C=C(C)c1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
44269089 103780 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 232 4 1 3 2.6 CC(Oc1ccccc1C(C)C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL266613 103780 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 232 4 1 3 2.6 CC(Oc1ccccc1C(C)C)C1=NCCN1 10.1016/j.bmc.2012.01.035
16757182 160030 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL397753 160030 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
16757182 160030 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL397753 160030 0 None 7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
11183468 116649 2 None -1 6 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL323402 116649 2 None -1 6 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
4567175 89251 5 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1021/jm060262x
CHEMBL217665 89251 5 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 318 3 1 4 3.7 CN1CCN(c2ccc(Nc3ccnc4ccccc34)cc2)CC1 10.1021/jm060262x
24906201 194132 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
CHEMBL493272 194132 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 280 2 1 4 2.5 c1ccc(-c2cccc3c2OCC(C2=NCCN2)O3)cc1 10.1021/jm800250z
1016 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -12 35 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
3157 8252 71 None -61 12 Human 6.1 pKi = 6.1 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
7170 8252 71 None -61 12 Human 6.1 pKi = 6.1 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
954 8252 71 None -61 12 Human 6.1 pKi = 6.1 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
CHEMBL707 8252 71 None -61 12 Human 6.1 pKi = 6.1 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
DB00590 8252 71 None -61 12 Human 6.1 pKi = 6.1 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1021/jm00018a001
56964693 80837 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 314 0 1 5 2.8 Clc1ccc2c(c1)N=C(N1CCNCC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022269 80837 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation countingDisplacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
ChEMBL 314 0 1 5 2.8 Clc1ccc2c(c1)N=C(N1CCNCC1)c1cccnc1O2 10.1021/jm2013419
12841596 124238 20 None 3 2 Bovine 7.1 pKi = 7.1 Binding
Binding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligandBinding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL2448004 124238 20 None 3 2 Bovine 7.1 pKi = 7.1 Binding
Binding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligandBinding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL339883 124238 20 None 3 2 Bovine 7.1 pKi = 7.1 Binding
Binding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligandBinding affinity against alpha-2 adrenergic receptor was determined in calf cerebral cortex homogenates using [3H]clonidine as radioligand
ChEMBL 237 1 1 5 0.8 Clc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
12909383 137481 1 None -5 2 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 278 0 0 2 3.6 CN1CCC(=C2c3ccccc3CCn3cccc32)CC1 10.1021/jm00361a008
CHEMBL368413 137481 1 None -5 2 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 278 0 0 2 3.6 CN1CCC(=C2c3ccccc3CCn3cccc32)CC1 10.1021/jm00361a008
44292470 108412 5 None 57 2 Bovine 7.1 pKi = 7.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 211 1 1 3 1.5 Cc1ccnc(N2CCNCC2)c1Cl 10.1021/jm00366a007
CHEMBL299007 108412 5 None 57 2 Bovine 7.1 pKi = 7.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 211 1 1 3 1.5 Cc1ccnc(N2CCNCC2)c1Cl 10.1021/jm00366a007
136044137 85712 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 472 6 1 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112976 85712 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 472 6 1 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CN2 10.1021/jm049619s
25130235 194366 1 None -2 11 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 194366 1 None -2 11 Human 7.1 pKi = 7.1 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
15675860 211208 0 None 4 4 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
CHEMBL72147 211208 0 None 4 4 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscineBinding affinity for human Alpha-2A adrenergic receptor from cultured LM(tk-) cells using [3H]rauwolscine
ChEMBL 305 1 2 5 2.1 Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1 10.1016/0960-894X(95)00391-6
23622576 179551 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
CHEMBL451229 179551 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 272 4 1 3 3.5 CC(Oc1ccccc1C1CCCCC1)C1=NCCN1 10.1021/jm800250z
3823 56995 42 None -40 11 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 56995 42 None -40 11 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 56995 42 None -40 11 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
1577 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
2537 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
5355 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
5501 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
643497 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
688272 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
958 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
960 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL196677 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL26 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
CHEMBL267044 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
DB00391 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
DB16021 10475 110 None -3 20 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N nan
10674896 213423 0 None -416 6 Human 6.1 pKi = 6.1 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 588 9 2 6 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1021/jm980077m
CHEMBL89243 213423 0 None -416 6 Human 6.1 pKi = 6.1 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 588 9 2 6 6.4 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(C#N)cc1 10.1021/jm980077m
657255 205863 34 None -10 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 205863 34 None -10 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
155567867 182812 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 502 8 0 6 5.7 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(-c4ccccc4)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4590209 182812 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 502 8 0 6 5.7 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(-c4ccccc4)cc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
10454026 24679 0 None -234 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
CHEMBL125916 24679 0 None -234 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
10895039 25292 0 None -51 7 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL127400 25292 0 None -51 7 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL129022 25292 0 None -51 7 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
10655607 211534 5 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 199 2 3 3 2.0 c1c[nH]c(Nc2ccc3[nH]cnc3c2)n1 10.1021/jm9605142
CHEMBL74544 211534 5 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 199 2 3 3 2.0 c1c[nH]c(Nc2ccc3[nH]cnc3c2)n1 10.1021/jm9605142
10326069 46070 1 None -42 9 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand.Binding affinity for recombinant human Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 46070 1 None -42 9 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand.Binding affinity for recombinant human Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
53324553 63629 0 None -10 10 Human 5.1 pKi = 5.1 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 63629 0 None -10 10 Human 5.1 pKi = 5.1 Binding
Inhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assayInhibition of adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
53324553 63629 0 None -10 10 Human 5.1 pKi = 5.1 Binding
Inhibition of alpha2A adrenergic receptorInhibition of alpha2A adrenergic receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 63629 0 None -10 10 Human 5.1 pKi = 5.1 Binding
Inhibition of alpha2A adrenergic receptorInhibition of alpha2A adrenergic receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
1210 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 7705 51 None -416 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
72947314 99265 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
CHEMBL2431281 99265 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 230 5 1 3 2.0 c1ccc(OCC2=NCCN2)c(CC2CC2)c1 10.1021/ml400232p
490 6979 8 None -758 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 6979 8 None -758 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 6979 8 None -758 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
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
12909389 67143 0 None -64 2 Bovine 4.1 pKi = 4.1 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 320 1 1 3 3.7 CN1CCC(=C2c3cc(C(=O)O)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
CHEMBL174649 67143 0 None -64 2 Bovine 4.1 pKi = 4.1 Binding
Displacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortexDisplacement of [3H]- clonidine radioligand binding at the alpha-2 adrenergic receptor binding site of calf cerebral cortex
ChEMBL 320 1 1 3 3.7 CN1CCC(=C2c3cc(C(=O)O)ccc3C=Cn3cccc32)CC1 10.1021/jm00361a008
16090598 89230 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 3 1 4 5.4 Cc1nc2cccc(Cl)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
CHEMBL217568 89230 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 394 3 1 4 5.4 Cc1nc2cccc(Cl)c2c(Nc2ccc(N3CCN(C)C(C)C3)cc2)c1C 10.1021/jm060262x
5467 212707 43 None -6 5 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC nan
CHEMBL84158 212707 43 None -6 5 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC nan
44288847 172088 0 None -5495 5 Human 5.1 pKi = 5.1 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL42335 172088 0 None -5495 5 Human 5.1 pKi = 5.1 Binding
In vivo inhibitory effect against Alpha-2A adrenergic receptorIn vivo inhibitory effect against Alpha-2A adrenergic receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
5897 111988 80 None -7 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 111988 80 None -7 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
44401164 76591 0 None -346 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 76591 0 None -346 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
90644744 119518 2 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 205 3 2 2 1.3 CCOc1ccc(N=C2NCCN2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289551 119518 2 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 205 3 2 2 1.3 CCOc1ccc(N=C2NCCN2)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304991 119518 2 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 205 3 2 2 1.3 CCOc1ccc(N=C2NCCN2)cc1 10.1016/j.ejmech.2014.05.057
16090623 89229 0 None -102 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
CHEMBL217567 89229 0 None -102 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
44415690 86912 0 None -363 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 86912 0 None -363 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
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
10923927 210957 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
CHEMBL70740 210957 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 279 3 2 5 0.8 O=S1(=O)CCCc2cccc(NCC3=NCCN3)c21 10.1021/jm000542r
6604789 107824 5 None -31 10 Human 5.1 pKi = 5.1 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL294649 107824 5 None -31 10 Human 5.1 pKi = 5.1 Binding
Binding affinity against Alpha-2A adrenergic receptorBinding affinity against Alpha-2A adrenergic receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
57399991 78023 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@H]2CO[C@H](C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
CHEMBL1956901 78023 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation countingDisplacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
ChEMBL 232 2 1 4 1.1 c1ccc([C@H]2CO[C@H](C3=NCCN3)CO2)cc1 10.1016/j.bmc.2012.02.016
12575 8769 30 None -5 17 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
54459 8769 30 None -5 17 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
CHEMBL10316 8769 30 None -5 17 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 10.1016/j.bmcl.2006.12.094
134987 193460 47 None 309 2 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 181 1 1 3 0.6 Fc1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL48833 193460 47 None 309 2 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 181 1 1 3 0.6 Fc1cccnc1N1CCNCC1 10.1021/jm00366a007
441975 23223 56 None -1 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
CHEMBL123325 23223 56 None -1 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 352 1 1 4 3.2 COC(=O)C1=CO[C@@H](C)[C@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 10.1021/jm00019a001
49864359 22398 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 467 10 1 5 4.1 COc1ccccc1N1CCN(CCCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
CHEMBL1221592 22398 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]MK912 from human alpha2A receptor after 60 minsDisplacement of [3H]MK912 from human alpha2A receptor after 60 mins
ChEMBL 467 10 1 5 4.1 COc1ccccc1N1CCN(CCCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.07.002
124 9755 47 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 9755 47 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 9755 47 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 9755 47 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 9755 47 None -4 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2803 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2012.06.008
516 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2012.06.008
704 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2012.06.008
CHEMBL134 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2012.06.008
DB00575 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1016/j.bmc.2012.06.008
10775000 114171 2 None -2 5 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 214 1 2 2 2.6 Oc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL317912 114171 2 None -2 5 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 214 1 2 2 2.6 Oc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
44324765 118345 0 None -2 5 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL328114 118345 0 None -2 5 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccccc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
9846548 214104 0 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL93489 214104 0 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 449 7 0 7 3.1 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccccc4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
1212 8443 50 None -165 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -165 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -165 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -165 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -165 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
9960497 107252 0 None -2454 6 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
CHEMBL290860 107252 0 None -2454 6 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.9 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)OCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm00010a001
16090628 148565 0 None -933 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1021/jm060262x
CHEMBL386169 148565 0 None -933 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 4 1 4 5.3 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(N2CCCN(C)CC2)cc1 10.1021/jm060262x
44574075 179355 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448802 179355 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
4601 213526 35 None -2 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 213526 35 None -2 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 213526 35 None -2 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
10466448 119660 2 None 34 2 Bovine 7.1 pKi = 7.1 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 0 5 0.8 Cc1cnc(N2CCN(C)CC2)c2nccn12 10.1021/jm00099a012
CHEMBL330994 119660 2 None 34 2 Bovine 7.1 pKi = 7.1 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 231 1 0 5 0.8 Cc1cnc(N2CCN(C)CC2)c2nccn12 10.1021/jm00099a012
44579229 196395 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 468 10 1 7 2.8 CCCCOc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
CHEMBL514837 196395 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 468 10 1 7 2.8 CCCCOc1ncccc1C(=O)NCCN1CCCN(CC2COc3ccccc3O2)CC1 10.1016/j.bmcl.2008.08.055
11000184 19824 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 19824 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 19824 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
10859076 20454 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 20454 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 20454 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
127036932 144126 0 None -2 22 Human 7.1 pKi = 7.1 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 144126 0 None -2 22 Human 7.1 pKi = 7.1 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
16757089 99066 1 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
CHEMBL242693 99066 1 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm061487a
16757089 99066 1 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
CHEMBL242693 99066 1 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 311 5 1 5 3.0 C[C@@H](Oc1ccccc1-c1cccc([N+](=O)[O-])c1)C1=NCCN1 10.1021/jm100977d
11448533 91466 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 0 3 3.6 CC(Oc1ccccc1-c1ccccc1)C1=NCCO1 10.1021/jm0408215
CHEMBL222591 91466 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 267 4 0 3 3.6 CC(Oc1ccccc1-c1ccccc1)C1=NCCO1 10.1021/jm0408215
11473729 91467 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 265 4 0 2 4.4 CC(Oc1ccccc1-c1ccccc1)C1=NCCC1 10.1021/jm0408215
CHEMBL222593 91467 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 265 4 0 2 4.4 CC(Oc1ccccc1-c1ccccc1)C1=NCCC1 10.1021/jm0408215
136680386 214482 0 None -169 6 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
44328801 214482 0 None -169 6 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
CHEMBL95578 214482 0 None -169 6 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 680 16 4 8 4.6 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(COCCCN)N1 10.1016/s0960-894x(99)00484-9
491 6980 9 None -1023 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 6980 9 None -1023 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 6980 9 None -1023 12 Human 7.1 pKi = 7.1 Binding
Ancillary Binding affinity towards cloned human Alpha-2A adrenergic receptorAncillary Binding affinity towards cloned human Alpha-2A adrenergic receptor
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
1530 8963 50 None -70 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 8963 50 None -70 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 8963 50 None -70 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 8963 50 None -70 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 8963 50 None -70 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3038495 7495 37 None -56 18 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
7625 7495 37 None -56 18 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
CHEMBL25236 7495 37 None -56 18 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
57345629 77960 0 None -5 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
CHEMBL1956197 77960 0 None -5 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1021/ml400232p
127036953 144293 0 None -8 22 Human 7.1 pKi = 7.1 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 144293 0 None -8 22 Human 7.1 pKi = 7.1 Binding
Binding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assayBinding affinity to alpha-2A adrenergic receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44269140 40327 0 None 4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 248 5 1 4 2.2 CC(C)Oc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL14208 40327 0 None 4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 248 5 1 4 2.2 CC(C)Oc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
57345629 77960 0 None -5 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956197 77960 0 None -5 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 246 5 1 4 2.0 CC(Oc1ccccc1OC1CC1)C1=NCCN1 10.1016/j.bmc.2012.01.035
9817231 165015 22 None 1 7 Human 5.1 pKi = 5.1 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
CHEMBL4088272 165015 22 None 1 7 Human 5.1 pKi = 5.1 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
90644755 119505 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 5 4 2 2.5 CCCNC(=N)Nc1ccc(NCC)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3289538 119505 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 5 4 2 2.5 CCCNC(=N)Nc1ccc(NCC)cc1 10.1016/j.ejmech.2014.05.057
CHEMBL3304668 119505 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 220 5 4 2 2.5 CCCNC(=N)Nc1ccc(NCC)cc1 10.1016/j.ejmech.2014.05.057
10044968 103320 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
CHEMBL262901 103320 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)C(C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
56852956 118820 1 None -218 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 118820 1 None -218 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL4642079 220802 0 None - 1 Human 5.1 pKi = 5.1 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
ChEMBL None None None Cc1c(N2CCNCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl 10.6019/CHEMBL4630901
9904606 16158 0 None 2 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 3 1 3 2.3 CN(c1cccc2c1CCCC2c1c[nH]cn1)S(C)(=O)=O 10.1021/jm030551a
CHEMBL111463 16158 0 None 2 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 305 3 1 3 2.3 CN(c1cccc2c1CCCC2c1c[nH]cn1)S(C)(=O)=O 10.1021/jm030551a
16090594 88900 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
CHEMBL216674 88900 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 388 3 1 4 5.4 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@@H](C)C4)cc3)c(C)c(C)nc2c1C 10.1021/jm060262x
56852956 118820 1 None -218 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 118820 1 None -218 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assayDisplacement of [3H]clonidine from human adrenergic-alpha2A receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL4642079 220802 0 None - 1 Human 5.1 pKi = 5.1 Binding
GPCRScan assay: inhibition of Alpha2AGPCRScan assay: inhibition of Alpha2A
ChEMBL None None None Cc1c(N2CCNCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl 10.6019/CHEMBL4630901
2803 7742 58 None -1 19 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
516 7742 58 None -1 19 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
704 7742 58 None -1 19 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
CHEMBL134 7742 58 None -1 19 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
DB00575 7742 58 None -1 19 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Alpha-2A adrenergic receptorBinding affinity towards Alpha-2A adrenergic receptor
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm990569e
2803 7742 58 None 1 19 Rat 6.1 pKi = 6.1 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
516 7742 58 None 1 19 Rat 6.1 pKi = 6.1 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
704 7742 58 None 1 19 Rat 6.1 pKi = 6.1 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
CHEMBL134 7742 58 None 1 19 Rat 6.1 pKi = 6.1 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
DB00575 7742 58 None 1 19 Rat 6.1 pKi = 6.1 Binding
in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligandin vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm000128r
237 211644 48 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 211644 48 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 211644 48 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 211644 48 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
11293787 154992 0 None -77 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 10.1016/j.bmcl.2006.12.094
CHEMBL393597 154992 0 None -77 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cellsDisplacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
ChEMBL 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 10.1016/j.bmcl.2006.12.094
155552185 180840 0 None -1548 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None -1548 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)Displacement of [3H] RX821002 from alpha2A adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
44582676 196558 0 None -6 17 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned alpha2A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha2A adrenergic receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 196558 0 None -6 17 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned alpha2A adrenergic receptor by competitive binding experimentInhibition of human cloned alpha2A adrenergic 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
10398419 123419 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1ccc2c(c1)CCC1(CN=CN1)C2 10.1021/jm00020a021
CHEMBL336970 123419 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligandBinding affinity towards Alpha-2A adrenergic receptor in human platelets using [3H]RX-821002 as radioligand
ChEMBL 216 1 1 3 1.6 COc1ccc2c(c1)CCC1(CN=CN1)C2 10.1021/jm00020a021
136019934 151308 0 None -7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
CHEMBL390718 151308 0 None -7 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 462 7 1 7 3.6 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C(C)=C/c4ccccc4)CC3)C1CN2 10.1016/j.bmc.2007.03.053
44350063 124726 0 None - 1 Bovine 6.1 pKi = 6.1 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 349 4 3 7 -0.0 C1=CN2CCN=C2C(N2CCNCC2)=N1.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
CHEMBL340358 124726 0 None - 1 Bovine 6.1 pKi = 6.1 Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
ChEMBL 349 4 3 7 -0.0 C1=CN2CCN=C2C(N2CCNCC2)=N1.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
11058166 211484 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 211484 0 None -2 5 Human 6.1 pKi = 6.1 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
9931977 69814 0 None -616 4 Human 6.1 pKi = 6.1 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
CHEMBL1788223 69814 0 None -616 4 Human 6.1 pKi = 6.1 Binding
Compound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosinCompound is evaluated for binding affinity towards Alpha-2A adrenergic receptor using [3H]prazosin
ChEMBL 421 4 0 7 3.3 COc1ccccc1N1CCN(C[C@H]2CN=C3c4ccccc4N=C(SC)N32)CC1 10.1021/jm970159v
132060763 169640 0 None -3 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4173095 169640 0 None -3 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Rauwolscine from human adrenergic alpha2A receptor expressed in stable MDCK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
44415593 87022 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 87022 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic alpha2A receptorBinding affinity at adrenergic alpha2A receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11732785 170499 0 None -18 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
CHEMBL420510 170499 0 None -18 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 bindingBinding affinity for rat cortex Alpha-2 adrenergic receptor was determined using [3H]-RX 81002 binding
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
10473701 90013 0 None -165 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1021/jm060262x
CHEMBL218679 90013 0 None -165 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 360 3 1 4 4.8 Cc1cnc2ccccc2c1Nc1ccc(N2CCN(C)C(C)(C)C2)cc1 10.1021/jm060262x
44424855 92229 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
CHEMBL226636 92229 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cellsDisplacement of [3H]rawolscine from human cloned adrenergic alpha2A receptor transfected in CHO cells
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NOC(CN3CCN(C/C=C/c4ccc(F)cc4)CC3)C1CO2 10.1016/j.bmc.2007.03.053
44330609 170231 0 None 2 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL419894 170231 0 None 2 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 467 7 0 7 3.3 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
135405894 85705 0 None -5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 470 8 1 8 2.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(CCOc4ccc(F)cc4)CC3)[C@@H]1CN2 10.1021/jm049619s
CHEMBL2112969 85705 0 None -5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity for alpha-2A adrenergic receptorBinding affinity for alpha-2A adrenergic receptor
ChEMBL 470 8 1 8 2.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(CCOc4ccc(F)cc4)CC3)[C@@H]1CN2 10.1021/jm049619s
10028898 118432 0 None -11 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(F)cc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
CHEMBL328631 118432 0 None -11 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity to the human alpha-2A adrenergic receptorIn vitro binding affinity to the human alpha-2A adrenergic receptor
ChEMBL 499 7 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C=C(\C)c4ccc(F)cc4F)CC3)[C@@H]1CO2 10.1016/j.bmcl.2004.03.031
123981 23231 22 None -2 8 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL123349 23231 22 None -2 8 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
CHEMBL536803 23231 22 None -2 8 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
ChEMBL 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 10.1021/jm00019a001
9816048 194057 0 None 12 3 Human 8.0 pKi = 8.0 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 231 1 4 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCN2 10.1021/jm960359r
CHEMBL49284 194057 0 None 12 3 Human 8.0 pKi = 8.0 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
ChEMBL 231 1 4 5 1.2 Cc1c(NC2=NCCN2)ccc2c1NCCN2 10.1021/jm960359r
463 8187 22 None -67 13 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
6918097 8187 22 None -67 13 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
837 8187 22 None -67 13 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
CHEMBL2051956 8187 22 None -67 13 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
DB14068 8187 22 None -67 13 Human 6.1 pKi = 6.1 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
ChEMBL 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C 10.1021/jm00010a001
16090627 88342 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1021/jm060262x
CHEMBL216197 88342 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 390 9 2 4 5.9 CCc1c(C)nc2c(C)cccc2c1Nc1ccc(NCCN(CC)CC)cc1 10.1021/jm060262x
2683 109665 25 None -12 16 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 109665 25 None -12 16 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 109665 25 None -12 16 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
10333157 158017 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
CHEMBL396013 158017 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm061487a
11140033 27455 0 None 7 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
CHEMBL130884 27455 0 None 7 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 265 4 2 3 3.2 CC(Nc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm0408215
10333157 158017 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
CHEMBL396013 158017 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 266 4 1 3 3.1 C[C@H](Oc1ccccc1-c1ccccc1)C1=NCCN1 10.1021/jm100977d
16090595 148179 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
CHEMBL383978 148179 0 None -109 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 374 3 1 4 5.0 Cc1ccc2c(Nc3ccc(N4CCN(C)[C@H](C)C4)cc3)c(C)c(C)nc2c1 10.1021/jm060262x
10651654 118260 0 None -489 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 631 9 2 5 7.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1021/jm980077m
CHEMBL327712 118260 0 None -489 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 631 9 2 5 7.8 CO/C(O)=C1\C(C)=NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc(Cl)c(Cl)c1 10.1021/jm980077m
10084076 104692 0 None -5 9 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Alpha-2 adrenergic receptorBinding affinity towards Alpha-2 adrenergic receptor
ChEMBL 262 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3N 10.1021/jm030030n
CHEMBL27251 104692 0 None -5 9 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Alpha-2 adrenergic receptorBinding affinity towards Alpha-2 adrenergic receptor
ChEMBL 262 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3N 10.1021/jm030030n
44324737 214017 0 None -2 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL92860 214017 0 None -2 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1016/s0960-894x(03)00525-0
44568614 194402 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 252 4 1 3 2.8 c1ccc(OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
CHEMBL494885 194402 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cellsDisplacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells
ChEMBL 252 4 1 3 2.8 c1ccc(OC(C2=NCCN2)c2ccccc2)cc1 10.1021/jm800250z
2337 10030 77 None -50 62 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 10030 77 None -50 62 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 10030 77 None -50 62 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 10030 77 None -50 62 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 10030 77 None -50 62 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5280805 92180 81 None -28 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 610 6 10 16 -1.7 C[C@@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(-c4ccc(O)c(O)c4)oc4cc(O)cc(O)c4c3=O)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@H](O)[C@H]1O 10.1021/np1000329
CHEMBL226335 92180 81 None -28 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
ChEMBL 610 6 10 16 -1.7 C[C@@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(-c4ccc(O)c(O)c4)oc4cc(O)cc(O)c4c3=O)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@H](O)[C@H]1O 10.1021/np1000329
25110718 200088 0 None -72 3 Human 7.0 pKi = 7.0 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(C[C@H]2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
CHEMBL524153 200088 0 None -72 3 Human 7.0 pKi = 7.0 Binding
Binding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assayBinding affinity at human recombinant adrenergic alpha2A receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 8 1 7 3.5 O=C(NCCN1CCCN(C[C@H]2COc3ccccc3O2)CC1)c1cccnc1Oc1ccccc1 10.1016/j.bmcl.2008.08.055
10527469 163044 3 None -204 16 Human 7.0 pKi = 7.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 163044 3 None -204 16 Human 7.0 pKi = 7.0 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine 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
164609730 191878 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4856060 191878 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of alpha2a adrenergic receptor (unknown origin)Inhibition of alpha2a adrenergic receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
71463022 90473 7 None 1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
CHEMBL2205362 90473 7 None 1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysisDisplacement of [3H]clonidine from alpha2A adrenergic receptor after 40 mins by scintillation counting analysis
ChEMBL 436 8 0 5 5.3 COc1cc2oc(C(=O)N(CCCN3CCCCC3)c3ccccc3)c(C)c2cc1OC 10.1016/j.bmc.2012.09.044
24841480 190678 0 None -47 20 Human 7.0 pKi = 7.0 Binding
Antagonist activity at adrenergic alpha2A receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 190678 0 None -47 20 Human 7.0 pKi = 7.0 Binding
Antagonist activity at adrenergic alpha2A receptor (unknown origin) by PDSP assayAntagonist activity at adrenergic alpha2A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
10489502 11290 2 None 6 3 Human 7.0 pKi = 7.0 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 227 2 2 2 3.5 Clc1cccc(Cl)c1Nc1ncc[nH]1 10.1021/jm9605142
CHEMBL1022 11290 2 None 6 3 Human 7.0 pKi = 7.0 Binding
Displacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cellsDisplacement of rauwolscine from human Alpha-2A adrenergic receptor expressed in CHO cells
ChEMBL 227 2 2 2 3.5 Clc1cccc(Cl)c1Nc1ncc[nH]1 10.1021/jm9605142
28918670 99262 2 None 4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
CHEMBL2431279 99262 2 None 4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human alpha2A ARBinding affinity at human alpha2A AR
ChEMBL 254 3 1 3 1.8 Brc1ccccc1OCC1=NCCN1 10.1021/ml400232p
10508132 113794 0 None -16 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1021/jm980077m
CHEMBL315392 113794 0 None -16 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 621 10 2 6 5.5 CC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)N(C)C)=C(C)N1 10.1021/jm980077m
10507651 213286 0 None -107 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
CHEMBL88388 213286 0 None -107 6 Human 6.0 pKi = 6.0 Binding
Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptorBinding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor
ChEMBL 591 9 2 6 5.8 CC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C1c1ccc2c(c1)OCO2 10.1021/jm980077m
9950711 115983 0 None -5 4 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL321644 115983 0 None -5 4 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1 10.1021/jm030551a
14004033 56006 5 None 2 2 Bovine 5.0 pKi = 5.0 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
CHEMBL156283 56006 5 None 2 2 Bovine 5.0 pKi = 5.0 Binding
Compound was evaluated for log 1/Ki at alpha-2 adrenergic receptorCompound was evaluated for log 1/Ki at alpha-2 adrenergic receptor
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
78114671 180943 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 350 6 0 6 2.5 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4546903 180943 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometryDisplacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
ChEMBL 350 6 0 6 2.5 CCOP(=O)(OCC)C1N=CC2C(=O)N(c3ccccc3)C(=O)C21 10.1021/acs.jmedchem.9b02080
44328654 113962 0 None -251 6 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 663 14 3 6 6.7 CCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL316495 113962 0 None -251 6 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 663 14 3 6 6.7 CCCC1=C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCC)=C(CC)N1 10.1016/s0960-894x(99)00484-9
21830793 98610 10 None -630 46 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 98610 10 None -630 46 Human 7.0 pKi = 7.0 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
139406787 183924 0 None 2 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4633982 183924 0 None 2 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to adrenergic alpha2A receptor (unknown origin)Binding affinity to adrenergic alpha2A receptor (unknown origin)
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
10251036 88660 0 None -162 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 410 4 2 5 4.7 CN1CCN(c2ccc(Nc3c(CO)cnc4cc(Cl)ccc34)cc2)CC1(C)C 10.1021/jm060262x
CHEMBL216464 88660 0 None -162 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 410 4 2 5 4.7 CN1CCN(c2ccc(Nc3c(CO)cnc4cc(Cl)ccc34)cc2)CC1(C)C 10.1021/jm060262x
14004033 56006 5 None 2 2 Bovine 5.0 pKi = 5.0 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
CHEMBL156283 56006 5 None 2 2 Bovine 5.0 pKi = 5.0 Binding
Affinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranesAffinity to alpha-2 adrenergic receptor by the displacement of [3H]clonidine from calf cerebral cortex membranes
ChEMBL 177 0 1 2 1.5 c1[nH]nc2c1CCN1CCCCC21 10.1021/jm00398a025
16090632 148494 0 None -46 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 348 4 3 5 3.3 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1 10.1021/jm060262x
CHEMBL385722 148494 0 None -46 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 348 4 3 5 3.3 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccccc34)cc2)CCN1 10.1021/jm060262x
2777786 181756 82 None 29 2 Bovine 7.0 pKi = 7.0 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1cccnc1N1CCNCC1 10.1021/jm00366a007
CHEMBL45663 181756 82 None 29 2 Bovine 7.0 pKi = 7.0 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1cccnc1N1CCNCC1 10.1021/jm00366a007
57399145 77959 0 None 7 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
CHEMBL1956196 77959 0 None 7 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
ChEMBL 234 5 1 4 1.9 CCOc1ccccc1OC(C)C1=NCCN1 10.1016/j.bmc.2012.01.035
49836307 25557 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
CHEMBL1278085 25557 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cellsDisplacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
ChEMBL 282 4 2 4 2.8 C[C@H](Oc1ccccc1-c1cccc(O)c1)C1=NCCN1 10.1021/jm100977d
9879119 16218 0 None -4 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1021/jm030551a
CHEMBL111771 16218 0 None -4 5 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assayIn vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1 10.1021/jm030551a
11747739 20007 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1191324 20007 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL542402 20007 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cellsAffinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44324860 214277 0 None -1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 479 6 0 8 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cc5ccccc5s4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
CHEMBL94435 214277 0 None -1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscineIn vitro binding affinity towards human alpha-2A adrenergic receptor using [3H]rauwolscine
ChEMBL 479 6 0 8 3.8 COc1cc2c(cc1OC)C1=NOC(CN3CCN(Cc4cc5ccccc5s4)CC3)C1CO2 10.1016/s0960-894x(03)00525-0
16090633 87236 0 None -25 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 380 4 2 5 3.8 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
CHEMBL214661 87236 0 None -25 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]rauwolscine from human ADRA2A expressed in S115 cellsDisplacement of [3H]rauwolscine from human ADRA2A expressed in S115 cells
ChEMBL 380 4 2 5 3.8 C[C@@H]1CN(c2ccc(Nc3c(CO)cnc4ccc(F)cc34)cc2)CCN1C 10.1021/jm060262x
4209 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 9937 75 None -1380 33 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
44329026 215204 0 None -19 6 Human 7.0 pKi = 7 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 679 16 3 7 6.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCOC)N1 10.1016/s0960-894x(99)00484-9
CHEMBL99864 215204 0 None -19 6 Human 7.0 pKi = 7 Binding
Binding affinity against human Alpha-2a adrenergic receptorBinding affinity against human Alpha-2a adrenergic receptor
ChEMBL 679 16 3 7 6.1 CCC1=C(C(N)=O)C(c2ccc([N+](=O)[O-])cc2)C(C(=O)NCCCN2CCC(c3ccccc3)(c3ccccc3)CC2)=C(CCCCOC)N1 10.1016/s0960-894x(99)00484-9
2105 9828 37 None -13 32 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 9828 37 None -13 32 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 9828 37 None -13 32 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 9828 37 None -13 32 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 9828 37 None -13 32 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
44574078 185540 0 None - 1 Human 6.0 pKi = 6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468711 185540 0 None - 1 Human 6.0 pKi = 6 Binding
Inhibition of adrenergic alpha2A receptorInhibition of adrenergic alpha2A receptor
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
168274641 197214 0 None - 1 Rat 5.0 pKi = 5 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 266 1 2 3 3.3 O=C1/C(=C/c2ccc(O)cc2)CCc2c(O)cccc21 10.1016/j.ejmech.2021.113964
CHEMBL5178192 197214 0 None - 1 Rat 5.0 pKi = 5 Binding
Displacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assayDisplacement of [3H]NECA from A2AAR in rat striata assessed as inhibition constant in presence of N6-cyclopentyladenosine by radioligand competitive binding assay
ChEMBL 266 1 2 3 3.3 O=C1/C(=C/c2ccc(O)cc2)CCc2c(O)cccc21 10.1016/j.ejmech.2021.113964
2477 7532 59 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 None - 29 Bovine 8.3 pIC50 = 8.3 Binding
Binding affinity against alpha-2 adrenergic receptor in calf frontal cortexBinding affinity against alpha-2 adrenergic receptor in calf frontal cortex
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
3689 109548 55 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligandCompound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
CHEMBL1372983 109548 55 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligandCompound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
CHEMBL305187 109548 55 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligandCompound was tested for the binding affinity against Alpha-1 adrenergic receptor by using [3H]prazosin as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
2803 7742 58 None - 19 Bovine 8.1 pIC50 = 8.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 None - 19 Bovine 8.1 pIC50 = 8.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 None - 19 Bovine 8.1 pIC50 = 8.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 None - 19 Bovine 8.1 pIC50 = 8.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 None - 19 Bovine 8.1 pIC50 = 8.1 Binding
Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
3294 8787 111 None - 44 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None - 44 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None - 44 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None - 44 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None - 44 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligandBinding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1795 8372 64 None - 1 Human 1.8 pKd = 1.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C 1325028
4186 8372 64 None - 1 Human 1.8 pKd = 1.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C 1325028
CHEMBL517986 8372 64 None - 1 Human 1.8 pKd = 1.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C 1325028
1192 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 1325028
1192 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 9584219
1794 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 1325028
1794 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 9584219
CHEMBL501701 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 1325028
CHEMBL501701 6935 47 None -51286 17 Human 2.5 pKd = 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 9584219
108094 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
108094 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
108094 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
526 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
526 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
526 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
528 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
528 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
528 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
CHEMBL10332 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
CHEMBL10332 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7908642
CHEMBL10332 10196 27 None -1 4 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 8819505
136 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
136 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
136 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8819505
223 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
223 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
223 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8819505
643606 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
643606 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
643606 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8819505
CHEMBL10347 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
CHEMBL10347 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
CHEMBL10347 10065 32 None -3 16 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8819505
2435 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
395 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
520 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
5386 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
CHEMBL844 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
DB00484 7509 100 None -2 12 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 2865672
1588 9105 27 3H-RX821002 1 44 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 3H-RX821002 1 44 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 3H-RX821002 1 44 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 3H-RX821002 1 44 Human 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 3H-RX821002 1 44 Human 10.3 pKi = 10.3 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
CHEMBL1196898 222809 0 3H-RAUWOLSCINE 1 3 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 248 3 1 5 1.2 CCOC1(COC2=CC=CC=C2O1)C3=NCCN3 None
2601 10552 33 3H-RX821002 -1 21 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 3H-RX821002 -1 21 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 3H-RX821002 -1 21 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 3H-RX821002 -1 21 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 3H-RX821002 -1 21 Human 9.5 pKi = 9.5 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
138107169 222731 0 3H-RAUWOLSCINE -6 23 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-RAUWOLSCINE -6 23 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
12576 7302 94 3H-RAUWOLSCINE -2 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
71310 7302 94 3H-RAUWOLSCINE -2 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
CHEMBL353972 7302 94 3H-RAUWOLSCINE -2 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
DB11481 7302 94 3H-RAUWOLSCINE -2 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 None
108094 10196 27 35S-GTPGammaS -1 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 10196 27 35S-GTPGammaS -1 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 10196 27 35S-GTPGammaS -1 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 10196 27 35S-GTPGammaS -1 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
None 222808 0 3H-RAUWOLSCINE -2 3 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 953 28 10 12 0.9 CCOC1=CC=C(C=C1)CC(C(=O)NC(CC2=CC=CC=C2)C(=O)NC(C(C)C)C(=O)NC(CC(=O)N)C(=O)NC(C=S)C(=O)NC(CCCCN)C(=O)N)NC(=O)CC3(CCCCC3)S None
138107169 222731 0 3H-RX821002 1 23 Pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-RX821002 1 23 Pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 222807 0 3H-RAUWOLSCINE -13 3 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 339 0 0 3 3.3 CN1CCC2(CCN3CCC4=C(C3C2)OC5=CC=CC=C45)N(C1=O)C None
138107169 222731 0 3H-RAUWOLSCINE -6 23 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-RAUWOLSCINE -6 23 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
102 10899 48 3H-RAUWOLSCINE -5 49 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-RAUWOLSCINE -5 49 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-RAUWOLSCINE -5 49 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-RAUWOLSCINE -5 49 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-RAUWOLSCINE -5 49 Human 9.3 pKi = 9.3 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
108094 10196 27 3H-MK912 -1 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
108094 10196 27 35S-GTPGammaS 1 4 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 10196 27 3H-MK912 -1 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 10196 27 35S-GTPGammaS 1 4 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 10196 27 3H-MK912 -1 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 10196 27 35S-GTPGammaS 1 4 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 10196 27 3H-MK912 -1 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 10196 27 35S-GTPGammaS 1 4 Mouse 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
102 10899 48 3H-RAUWOLSCINE -5 49 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-RAUWOLSCINE -5 49 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-RAUWOLSCINE -5 49 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-RAUWOLSCINE -5 49 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-RAUWOLSCINE -5 49 Human 9.2 pKi = 9.2 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
164512323 222810 0 3H-RAUWOLSCINE -5 5 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RAUWOLSCINE -5 5 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
124 9755 47 3H-RAUWOLSCINE -4 32 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RAUWOLSCINE -4 32 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RAUWOLSCINE -4 32 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RAUWOLSCINE -4 32 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RAUWOLSCINE -4 32 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 222737 0 3H-RAUWOLSCINE -14 19 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
108094 10196 27 3H-RAUWOLSCINE -1 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 10196 27 3H-RAUWOLSCINE -1 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 10196 27 3H-RAUWOLSCINE -1 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 10196 27 3H-RAUWOLSCINE -1 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
None 222740 0 3H-RAUWOLSCINE -1 5 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 295 5 2 3 3.0 C1CC2=CC=CC=C2C(=O)C1CNCCC3=CC=C(C=C3)O None
None 222737 0 3H-RX821002 -6 19 Pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
108094 10196 27 3H-MK912 -1 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
526 10196 27 3H-MK912 -1 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
528 10196 27 3H-MK912 -1 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
CHEMBL10332 10196 27 3H-MK912 -1 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 None
138107169 222731 0 35S-GTPGammaS -6 23 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 35S-GTPGammaS -6 23 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 222737 0 3H-RAUWOLSCINE -14 19 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
41 8440 0 3H-PRAZOSIN -1 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-PRAZOSIN -1 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-PRAZOSIN -1 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
None 222737 0 3H-RAUWOLSCINE -14 19 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
124 9755 47 3H-RAUWOLSCINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RAUWOLSCINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RAUWOLSCINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RAUWOLSCINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RAUWOLSCINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
124 9755 47 3H-CLONIDINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-CLONIDINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-CLONIDINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-CLONIDINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-CLONIDINE -4 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
124 9755 47 3H-RAUWOLSCINE -4 32 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RAUWOLSCINE -4 32 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RAUWOLSCINE -4 32 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RAUWOLSCINE -4 32 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RAUWOLSCINE -4 32 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2142 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RX821002 -2 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
102 10899 48 3H-RAUWOLSCINE -5 49 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-RAUWOLSCINE -5 49 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-RAUWOLSCINE -5 49 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-RAUWOLSCINE -5 49 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-RAUWOLSCINE -5 49 Human 8.8 pKi = 8.8 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
None 223486 0 UNDEFINED 1 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 390 1 2 4 3.1 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O.Cl None
12575 8769 30 3H-RAUWOLSCINE -5 17 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 8769 30 3H-RAUWOLSCINE -5 17 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 8769 30 3H-RAUWOLSCINE -5 17 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
2389 10104 118 3H-RAUWOLSCINE -77 66 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-RAUWOLSCINE -77 66 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-RAUWOLSCINE -77 66 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-RAUWOLSCINE -77 66 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-RAUWOLSCINE -77 66 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
164512323 222810 0 3H-RX821002 -18 5 Pig 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RX821002 -18 5 Pig 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
46780481 114308 20 3H-CLONIDINE -47 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-CLONIDINE -47 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-CLONIDINE -47 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-CLONIDINE -47 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
521 8186 69 None -2 7 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
5311068 8186 69 None -2 7 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
835 8186 69 None -2 7 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
CHEMBL778 8186 69 None -2 7 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
DB00633 8186 69 None -2 7 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C None
31101 7516 40 3H-RX821002 -10 35 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-RX821002 -10 35 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-RX821002 -10 35 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-RX821002 -10 35 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-RX821002 -10 35 Human 8.0 pKi = 8.0 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
202 8290 77 UNDEFINED -9 33 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 8290 77 UNDEFINED -9 33 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 8290 77 UNDEFINED -9 33 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 8290 77 UNDEFINED -9 33 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 8290 77 UNDEFINED -9 33 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
104870 105656 47 3H-Yohimbine -54 21 Pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 3H-Yohimbine -54 21 Pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 3H-Yohimbine -54 21 Pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5656 209845 87 UNDEFINED -25 43 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 UNDEFINED -25 43 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 209906 52 UNDEFINED -1 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 209906 52 UNDEFINED -1 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
165193 222724 0 3H-RAUWOLSCINE -4265 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-RAUWOLSCINE -4265 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-RAUWOLSCINE -4265 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
3075702 224111 0 3H-RAUWOLSCINE -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1499 8872 47 35S-GTPGammaS -1445 17 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1499 8872 47 3H-Yohimbine -1445 17 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 35S-GTPGammaS -1445 17 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 3H-Yohimbine -1445 17 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 35S-GTPGammaS -1445 17 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 3H-Yohimbine -1445 17 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 35S-GTPGammaS -1445 17 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 3H-Yohimbine -1445 17 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 35S-GTPGammaS -1445 17 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 3H-Yohimbine -1445 17 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
243 9976 91 3H-RAUWOLSCINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 3H-RAUWOLSCINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 3H-RAUWOLSCINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 3H-RAUWOLSCINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 3H-RAUWOLSCINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 10035 23 3H-RX821002 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-RX821002 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-RX821002 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
183782 10171 20 3H-RAUWOLSCINE -2398 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
237 10171 20 3H-RAUWOLSCINE -2398 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL85251 10171 20 3H-RAUWOLSCINE -2398 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
6917970 10463 61 3H-CLONIDINE -2290 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 10463 61 3H-CLONIDINE -2290 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 10463 61 3H-CLONIDINE -2290 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
2662 18156 131 3H-CLONIDINE -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 3H-CLONIDINE -41 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
5090 22333 106 3H-CLONIDINE -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 3H-CLONIDINE -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
127151 42104 18 3H-RX821002 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
3022645 42104 18 3H-RX821002 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
CHEMBL14370 42104 18 3H-RX821002 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
156391 53574 99 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 53574 99 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 53574 99 3H-CLONIDINE -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
10624 77075 19 125I-Clonidine -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 77075 19 125I-Clonidine -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 77075 19 125I-Clonidine -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 101008 100 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 101008 100 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 106743 83 3H-CLONIDINE -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 106743 83 3H-CLONIDINE -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 140299 14 3H-CLONIDINE -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 3H-CLONIDINE -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
5280343 195054 124 3H-CLONIDINE -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 3H-CLONIDINE -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 3H-CLONIDINE -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
3672 199312 136 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 199312 136 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 200394 112 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 200394 112 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
2771 201796 74 3H-RAUWOLSCINE -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 201796 74 3H-RX821002 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-RAUWOLSCINE -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-RX821002 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-RAUWOLSCINE -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-RX821002 -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
4495 203314 92 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 203314 92 3H-CLONIDINE -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
54677470 207330 115 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 207330 115 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 207330 115 3H-CLONIDINE -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
5281600 209804 92 3H-CLONIDINE -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-CLONIDINE -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 209845 87 3H-RX821002 -25 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 3H-RX821002 -25 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
4054 212280 72 125I-Clonidine -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 125I-Clonidine -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 125I-Clonidine -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
119607 212982 113 3H-CLONIDINE -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 212982 113 3H-CLONIDINE -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
None 222772 0 3H-RAUWOLSCINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 222798 0 3H-CLONIDINE -41686 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 222806 0 3H-RAUWOLSCINE -6309 13 Rat 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
25137849 222958 0 3H-CLONIDINE -2 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-CLONIDINE -2 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
31404 222972 0 3H-Yohimbine - 1 Pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 253 1 1 4 1.5 CCN1CCC2=C(CC1)OC(=N2)N.Cl.Cl None
None 223090 0 3H-CLONIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 223091 0 3H-CLONIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-CLONIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 223093 0 3H-CLONIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 223094 0 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 223095 0 3H-CLONIDINE -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 3H-CLONIDINE -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223097 0 3H-CLONIDINE -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 223106 0 3H-CLONIDINE -16 27 Human 5.0 pKi = 5 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
4978 223107 0 3H-CLONIDINE -7 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 223108 0 3H-CLONIDINE 2 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 223110 0 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 223121 0 3H-RX821002 -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 223168 0 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 223169 0 3H-CLONIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 223170 0 3H-CLONIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 223171 0 3H-CLONIDINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 223172 0 3H-CLONIDINE -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 223173 0 3H-CLONIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 223174 0 3H-CLONIDINE -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 223268 0 3H-CLONIDINE -4570 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
11954224 222732 0 3H-CLONIDINE -446 59 Human 7.0 pKi = 7.0 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
1830 9368 44 3H-CLONIDINE -14 28 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-CLONIDINE -14 28 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-CLONIDINE -14 28 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-CLONIDINE -14 28 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-CLONIDINE -14 28 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
None 222811 0 3H-RAUWOLSCINE -19 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 401 6 1 5 0.6 CS(=O)(=O)NCCN(C1CCN2CCC3=CC=CC=C3C2C1)S(=O)(=O)C None
11079 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 9510 63 35S-GTPGammaS 1 5 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
179 7188 115 125I-Clonidine -35 50 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 125I-Clonidine -35 50 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 125I-Clonidine -35 50 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 125I-Clonidine -35 50 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 125I-Clonidine -35 50 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
1353 8692 93 3H-CLONIDINE -190 85 Human 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
1353 8692 93 3H-RAUWOLSCINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-CLONIDINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-RAUWOLSCINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-CLONIDINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-RAUWOLSCINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-CLONIDINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-RAUWOLSCINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-CLONIDINE -190 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-RAUWOLSCINE -190 85 Human 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
4209 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 3H-RX821002 -794 33 Pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
None 223120 0 3H-RX821002 -15 19 Human 7.9 pKi = 7.9 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
1267 10576 49 3H-RAUWOLSCINE -52 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 10576 49 3H-RAUWOLSCINE -52 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 10576 49 3H-RAUWOLSCINE -52 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
None 223158 0 3H-RAUWOLSCINE -141 11 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
5268 10428 40 3H-RAUWOLSCINE -63 18 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-RAUWOLSCINE -63 18 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-RAUWOLSCINE -63 18 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
68602 211905 80 35S-GTPGammaS -1 8 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 211905 80 35S-GTPGammaS -1 8 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
164512323 222810 0 3H-RAUWOLSCINE -5 5 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RAUWOLSCINE -5 5 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
122211 7250 0 3H-RAUWOLSCINE -239 6 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 7250 0 3H-RAUWOLSCINE -239 6 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
138107169 222731 0 3H-RAUWOLSCINE -6 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-RAUWOLSCINE -6 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
122211 7250 0 3H-MK912 -239 6 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 7250 0 3H-MK912 -239 6 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
10297 33885 30 3H-CLONIDINE -5 43 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 3H-CLONIDINE -5 43 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
100 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-CLONIDINE -33 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44438148 100265 0 UNDEFINED -14 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 None
CHEMBL246229 100265 0 UNDEFINED -14 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 430 6 0 6 5.1 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccn4)cc13)CC2 None
135409468 8816 69 3H-CLONIDINE -48 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-CLONIDINE -48 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-CLONIDINE -48 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
2995 211184 53 3H-RAUWOLSCINE -12 23 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 3H-RAUWOLSCINE -12 23 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 3H-RAUWOLSCINE -12 23 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
None 222737 0 3H-MK912 -14 19 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
164512323 222810 0 3H-RX821002 -18 5 Pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RX821002 -18 5 Pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
44438166 100592 0 UNDEFINED -33 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 467 8 2 7 3.5 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCC(C)(C)N)cc13)CC2 None
CHEMBL247664 100592 0 UNDEFINED -33 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 467 8 2 7 3.5 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCC(C)(C)N)cc13)CC2 None
25058166 222739 0 3H-RX821002 -70 26 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-RX821002 -70 26 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
484 9633 51 35S-GTPGammaS -14 35 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 35S-GTPGammaS -14 35 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 35S-GTPGammaS -14 35 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
135398737 7745 93 3H-CLONIDINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-RAUWOLSCINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-CLONIDINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-RAUWOLSCINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-CLONIDINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-RAUWOLSCINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-CLONIDINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-RAUWOLSCINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-CLONIDINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-RAUWOLSCINE -26 90 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
7153 104796 77 3H-CLONIDINE -7 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-CLONIDINE -7 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1028 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 35S-GTPGammaS -48 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
3658 10879 53 35S-GTPGammaS -5 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 10879 53 35S-GTPGammaS -5 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 10879 53 35S-GTPGammaS -5 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 10879 53 35S-GTPGammaS -5 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 10879 53 35S-GTPGammaS -5 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
124 9755 47 35S-GTPGammaS -28 32 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 35S-GTPGammaS -28 32 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 35S-GTPGammaS -28 32 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 35S-GTPGammaS -28 32 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 35S-GTPGammaS -28 32 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
5524 223243 0 35S-GTPGammaS -1 4 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 215 1 2 3 1.9 C1CCC2=C(C1)C=CC=C2NC3=NCCN3 None
68602 211905 80 3H-MK912 -1 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 211905 80 3H-MK912 -1 8 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
1613 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2389 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1613 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-CLONIDINE -8 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2389 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-CLONIDINE -77 66 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
68712 107114 60 35S-GTPGammaS -1 5 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
CHEMBL289480 107114 60 35S-GTPGammaS -1 5 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
186 8588 52 3H-CLONIDINE -263 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 8588 52 3H-CLONIDINE -263 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 8588 52 3H-CLONIDINE -263 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
16362 9899 71 3H-CLONIDINE -501 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-CLONIDINE -501 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-CLONIDINE -501 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-CLONIDINE -501 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-CLONIDINE -501 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
11079 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 9510 63 35S-GTPGammaS 1 5 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
2865 10915 73 3H-CLONIDINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 10915 73 3H-RAUWOLSCINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-CLONIDINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-RAUWOLSCINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-CLONIDINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-RAUWOLSCINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-CLONIDINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-RAUWOLSCINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-CLONIDINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-RAUWOLSCINE -64 53 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
3294 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3294 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-RX821002 -47 44 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
119570 9933 96 3H-RX821002 -41 39 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-RX821002 -41 39 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-RX821002 -41 39 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-RX821002 -41 39 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-RX821002 -41 39 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
1223 7740 41 3H-RAUWOLSCINE -93 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 7740 41 3H-RAUWOLSCINE -93 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 7740 41 3H-RAUWOLSCINE -93 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
134 9292 24 3H-CLONIDINE -74 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-CLONIDINE -74 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-CLONIDINE -74 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-CLONIDINE -74 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-CLONIDINE -74 67 Human 6.8 pKi = 6.8 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
122211 7250 0 3H-RAUWOLSCINE -239 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 7250 0 3H-RAUWOLSCINE -239 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
16725934 154201 0 UNDEFINED -87 3 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 None
CHEMBL392992 154201 0 UNDEFINED -87 3 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 429 6 0 5 5.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4)cc13)CC2 None
15897 9637 0 3H-CLONIDINE -134 36 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-CLONIDINE -134 36 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-CLONIDINE -134 36 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
103 10925 61 3H-RAUWOLSCINE -54 53 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-RAUWOLSCINE -54 53 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-RAUWOLSCINE -54 53 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-RAUWOLSCINE -54 53 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-RAUWOLSCINE -54 53 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 3H-CLONIDINE -87 72 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-CLONIDINE -87 72 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-CLONIDINE -87 72 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-CLONIDINE -87 72 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-CLONIDINE -87 72 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1220 6975 55 3H-RAUWOLSCINE -147 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-RAUWOLSCINE -147 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-RAUWOLSCINE -147 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-RAUWOLSCINE -147 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
44438168 100593 0 UNDEFINED -53 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 533 7 0 7 4.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)N4CCC(N5CCCC5)CC4)cc13)CC2 None
CHEMBL247665 100593 0 UNDEFINED -53 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 533 7 0 7 4.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)N4CCC(N5CCCC5)CC4)cc13)CC2 None
2402 10143 62 3H-RX821002 -5 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-RX821002 -5 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-RX821002 -5 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-RX821002 -5 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-RX821002 -5 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
2142 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RX821002 -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
185 10778 60 3H-CLONIDINE -5888 37 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-CLONIDINE -5888 37 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-CLONIDINE -5888 37 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-CLONIDINE -5888 37 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
135398745 9688 112 3H-RAUWOLSCINE -93 65 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-RAUWOLSCINE -93 65 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-RAUWOLSCINE -93 65 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-RAUWOLSCINE -93 65 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
484 9633 51 35S-GTPGammaS -9 35 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 35S-GTPGammaS -9 35 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 35S-GTPGammaS -9 35 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
68602 211905 80 35S-GTPGammaS -1 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 211905 80 35S-GTPGammaS -1 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
None 222738 0 3H-RAUWOLSCINE -2 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 358 4 0 3 2.8 CCCS(=O)(=O)N(C)C1CCN2CCC3=CC=CC=C3C2C1.Cl None
123981 23231 22 3H-RAUWOLSCINE -2 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
CHEMBL123349 23231 22 3H-RAUWOLSCINE -2 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
CHEMBL536803 23231 22 3H-RAUWOLSCINE -2 8 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 195 0 0 1 2.4 CN1CCc2cccc(Cl)c2CC1 None
2142 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RAUWOLSCINE -2 37 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RX821002 -1 37 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
1816 9318 102 3H-RAUWOLSCINE -51 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 9318 102 3H-RAUWOLSCINE -51 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 9318 102 3H-RAUWOLSCINE -51 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 9318 102 3H-RAUWOLSCINE -51 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 9318 102 3H-RAUWOLSCINE -51 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
1343 8670 62 35S-GTPGammaS -3 9 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 8670 62 35S-GTPGammaS -3 9 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 8670 62 35S-GTPGammaS -3 9 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 8670 62 35S-GTPGammaS -3 9 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 8670 62 35S-GTPGammaS -3 9 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
2142 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 35S-GTPGammaS -2 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
11079 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 9510 63 35S-GTPGammaS -1 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
25137849 222958 0 3H-CLONIDINE -2 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-CLONIDINE -2 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
11750482 154199 0 UNDEFINED -25 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 None
CHEMBL392991 154199 0 UNDEFINED -25 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 419 6 0 6 5.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccco4)cc13)CC2 None
3952 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 8669 38 35S-GTPGammaS -3 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
2435 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 7509 100 35S-GTPGammaS -2 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
4209 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 3H-RAUWOLSCINE -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
44438161 153919 0 UNDEFINED -22 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 543 10 1 7 5.0 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4cccc(C(=O)NCCN(C)C)c4)cc13)CC2 None
CHEMBL392771 153919 0 UNDEFINED -22 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 543 10 1 7 5.0 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4cccc(C(=O)NCCN(C)C)c4)cc13)CC2 None
2337 10030 77 3H-RAUWOLSCINE -50 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-RAUWOLSCINE -50 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-RAUWOLSCINE -50 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-RAUWOLSCINE -50 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-RAUWOLSCINE -50 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
4209 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 3H-MK912 -1380 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
2695 10613 81 35S-GTPGammaS -9 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 10613 81 35S-GTPGammaS -9 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 10613 81 35S-GTPGammaS -9 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 10613 81 35S-GTPGammaS -9 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 10613 81 35S-GTPGammaS -9 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
2389 10104 118 3H-RAUWOLSCINE -77 66 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-RAUWOLSCINE -77 66 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-RAUWOLSCINE -77 66 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-RAUWOLSCINE -77 66 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-RAUWOLSCINE -77 66 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3658 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
103 10925 61 3H-CLONIDINE -54 53 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-CLONIDINE -54 53 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-CLONIDINE -54 53 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-CLONIDINE -54 53 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-CLONIDINE -54 53 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
523 10878 93 35S-GTPGammaS 1 5 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
5707 10878 93 35S-GTPGammaS 1 5 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
CHEMBL297362 10878 93 35S-GTPGammaS 1 5 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
DB11477 10878 93 35S-GTPGammaS 1 5 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
135398737 7745 93 3H-RAUWOLSCINE -26 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-RAUWOLSCINE -26 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-RAUWOLSCINE -26 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-RAUWOLSCINE -26 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-RAUWOLSCINE -26 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2695 10613 81 3H-RAUWOLSCINE -9 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 10613 81 3H-RAUWOLSCINE -9 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 10613 81 3H-RAUWOLSCINE -9 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 10613 81 3H-RAUWOLSCINE -9 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 10613 81 3H-RAUWOLSCINE -9 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
2803 7742 58 3H-RX821002 1 19 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 3H-RX821002 1 19 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 3H-RX821002 1 19 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 3H-RX821002 1 19 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 3H-RX821002 1 19 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
124 9755 47 35S-GTPGammaS -28 32 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 35S-GTPGammaS -28 32 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 35S-GTPGammaS -28 32 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 35S-GTPGammaS -28 32 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 35S-GTPGammaS -28 32 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
3658 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 10879 53 35S-GTPGammaS -9 8 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
2726 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1615 174570 24 3H-CLONIDINE -6 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-CLONIDINE -6 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2726 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-RAUWOLSCINE -87 72 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
44438152 100383 0 UNDEFINED -134 3 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 None
CHEMBL246639 100383 0 UNDEFINED -134 3 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 459 7 0 6 5.7 COc1cccc(-c2cc3c(CN4CCc5cc(OC)c(OC)cc5C4)ccc(OC)c3o2)c1 None
162265 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
162265 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-CLONIDINE -12 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5268 10428 40 3H-RAUWOLSCINE -63 18 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-RAUWOLSCINE -63 18 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-RAUWOLSCINE -63 18 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
None 223018 0 3H-CLONIDINE -30199 29 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
2216 7234 50 3H-Yohimbine -57 6 Pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
229 7234 50 3H-Yohimbine -57 6 Pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
7117 7234 50 3H-Yohimbine -57 6 Pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
CHEMBL647 7234 50 3H-Yohimbine -57 6 Pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
DB00964 7234 50 3H-Yohimbine -57 6 Pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
102 10899 48 3H-RX821002 -5 49 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-RX821002 -5 49 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-RX821002 -5 49 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-RX821002 -5 49 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-RX821002 -5 49 Human 8.5 pKi = 8.5 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
68602 211905 80 3H-RX821002 -1 8 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 211905 80 3H-RX821002 -1 8 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
124 9755 47 3H-RX821002 -16 32 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RX821002 -16 32 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RX821002 -16 32 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RX821002 -16 32 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RX821002 -16 32 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
124 9755 47 3H-RAUWOLSCINE -4 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RAUWOLSCINE -4 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RAUWOLSCINE -4 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RAUWOLSCINE -4 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RAUWOLSCINE -4 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
5268 10428 40 3H-RX821002 -10 18 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-RX821002 -10 18 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-RX821002 -10 18 Pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
68602 211905 80 35S-GTPGammaS 1 8 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
CHEMBL77921 211905 80 35S-GTPGammaS 1 8 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 200 2 1 1 3.2 Cc1cccc(C(C)c2c[nH]cn2)c1C None
138107169 222731 0 3H-RAUWOLSCINE -6 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-RAUWOLSCINE -6 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 222737 0 3H-RAUWOLSCINE -14 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
102 10899 48 3H-MK912 -5 49 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-MK912 -5 49 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-MK912 -5 49 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-MK912 -5 49 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-MK912 -5 49 Human 8.4 pKi = 8.4 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
138107169 222731 0 3H-MK912 -6 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-MK912 -6 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
115237 62359 119 3H-RAUWOLSCINE -44 54 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-RAUWOLSCINE -44 54 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
122295 16640 7 3H-RAUWOLSCINE -1 9 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
CHEMBL114166 16640 7 3H-RAUWOLSCINE -1 9 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
4209 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
162265 209053 22 3H-CLONIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-CLONIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-CLONIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
1212 8443 50 3H-RAUWOLSCINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-RAUWOLSCINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-RAUWOLSCINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-RAUWOLSCINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-RAUWOLSCINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11225732 100432 0 UNDEFINED -16 3 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 None
CHEMBL246852 100432 0 UNDEFINED -16 3 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 497 6 0 5 6.7 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4C(F)(F)F)cc13)CC2 None
2803 7742 58 3H-RX821002 -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 3H-RX821002 -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 3H-RX821002 -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 3H-RX821002 -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 3H-RX821002 -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
5524 223243 0 35S-GTPGammaS 1 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 215 1 2 3 1.9 C1CCC2=C(C1)C=CC=C2NC3=NCCN3 None
1212 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1212 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-CLONIDINE -165 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-CLONIDINE -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4209 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 3H-RAUWOLSCINE -1380 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
133621 8793 0 35S-GTPGammaS -6 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
3470 8793 0 35S-GTPGammaS -6 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
CHEMBL347695 8793 0 35S-GTPGammaS -6 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 244 3 0 4 2.3 CCn1ccnc1CC1COc2c(O1)cccc2 None
523 10878 93 3H-Yohimbine -1 5 Pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
5707 10878 93 3H-Yohimbine -1 5 Pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
CHEMBL297362 10878 93 3H-Yohimbine -1 5 Pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
DB11477 10878 93 3H-Yohimbine -1 5 Pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
122295 16640 7 3H-RAUWOLSCINE -1 9 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
CHEMBL114166 16640 7 3H-RAUWOLSCINE -1 9 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
None 223018 0 3H-CLONIDINE -30199 29 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
122295 16640 7 3H-RX821002 -1 9 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
CHEMBL114166 16640 7 3H-RX821002 -1 9 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 3.7 CC(C)=CCOc1ccc(Cl)c2c1CCN(C)CC2 None
2803 7742 58 35S-GTPGammaS -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 35S-GTPGammaS -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 35S-GTPGammaS -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 35S-GTPGammaS -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 35S-GTPGammaS -1 19 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
124 9755 47 3H-Yohimbine -16 32 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-Yohimbine -16 32 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-Yohimbine -16 32 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-Yohimbine -16 32 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-Yohimbine -16 32 Pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
138107169 222731 0 35S-GTPGammaS -97 23 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 35S-GTPGammaS -97 23 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2337 10030 77 125I-Clonidine -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 10030 77 3H-CLONIDINE -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 125I-Clonidine -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-CLONIDINE -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 125I-Clonidine -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-CLONIDINE -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 125I-Clonidine -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-CLONIDINE -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 125I-Clonidine -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-CLONIDINE -50 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
122211 7250 0 3H-RX821002 -229 6 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 7250 0 3H-RX821002 -229 6 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
104870 105656 47 3H-RX821002 -2 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 3H-RX821002 -2 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 3H-RX821002 -2 21 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
484 9633 51 3H-RX821002 -14 35 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-RX821002 -14 35 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-RX821002 -14 35 Pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
1524 8962 96 3H-RAUWOLSCINE -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-RAUWOLSCINE -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-RAUWOLSCINE -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-RAUWOLSCINE -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-RAUWOLSCINE -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-RAUWOLSCINE -281 51 Human 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
122211 7250 0 3H-RAUWOLSCINE -239 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
524 7250 0 3H-RAUWOLSCINE -239 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C None
3337 213146 27 3H-CLONIDINE -27 40 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-CLONIDINE -27 40 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-CLONIDINE -27 40 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-CLONIDINE -27 40 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-CLONIDINE -27 40 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
67409 222813 0 3H-RAUWOLSCINE -7 3 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 235 2 0 1 3.9 C=CCN1CC2=CC=CC=C2C3=CC=CC=C3C1 None
8966 222813 0 3H-RAUWOLSCINE -7 3 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 235 2 0 1 3.9 C=CCN1CC2=CC=CC=C2C3=CC=CC=C3C1 None
1028 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 35S-GTPGammaS -72 30 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
484 9633 51 35S-GTPGammaS -9 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 35S-GTPGammaS -9 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 35S-GTPGammaS -9 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
104870 105656 47 35S-GTPGammaS -2 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 35S-GTPGammaS -2 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 35S-GTPGammaS -2 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
24840389 121991 4 3H-RX821002 -295 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 121991 4 3H-RX821002 -295 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
2142 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RAUWOLSCINE -2 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
931 223242 0 35S-GTPGammaS -1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 128 0 0 0 2.8 C1=CC=C2C=CC=CC2=C1 None
115237 62359 119 3H-CLONIDINE -44 54 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-CLONIDINE -44 54 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
12057539 214820 42 None -9 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 214820 42 None -9 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 214820 42 None -9 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
124 9755 47 3H-RAUWOLSCINE -4 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-RAUWOLSCINE -4 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-RAUWOLSCINE -4 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-RAUWOLSCINE -4 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-RAUWOLSCINE -4 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2803 7742 58 35S-GTPGammaS -3 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 35S-GTPGammaS -3 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 35S-GTPGammaS -3 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 35S-GTPGammaS -3 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 35S-GTPGammaS -3 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
44438147 100264 0 UNDEFINED -20 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 None
CHEMBL246228 100264 0 UNDEFINED -20 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 406 5 1 9 2.5 COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2 None
10836 21239 14 3H-CLONIDINE -2 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 21239 14 3H-CLONIDINE -2 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
44438167 155749 0 UNDEFINED -52 3 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 None
CHEMBL394218 155749 0 UNDEFINED -52 3 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 505 7 1 7 3.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NC4CN5CCC4CC5)cc13)CC2 None
2435 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 7509 100 35S-GTPGammaS -7 12 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
100 10577 58 3H-RAUWOLSCINE -33 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-RAUWOLSCINE -33 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-RAUWOLSCINE -33 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-RAUWOLSCINE -33 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-RAUWOLSCINE -33 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44438165 173563 0 UNDEFINED -48 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 467 9 1 7 3.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCCN(C)C)cc13)CC2 None
CHEMBL428407 173563 0 UNDEFINED -48 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 467 9 1 7 3.3 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(C(=O)NCCN(C)C)cc13)CC2 None
135 9310 43 3H-RAUWOLSCINE -4 56 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-RAUWOLSCINE -4 56 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-RAUWOLSCINE -4 56 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-RAUWOLSCINE -4 56 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-RAUWOLSCINE -4 56 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
164512323 222810 0 3H-RAUWOLSCINE -5 5 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RAUWOLSCINE -5 5 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
135398745 9688 112 3H-RAUWOLSCINE -93 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-RAUWOLSCINE -93 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-RAUWOLSCINE -93 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-RAUWOLSCINE -93 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1353 8692 93 3H-RAUWOLSCINE -190 85 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-RAUWOLSCINE -190 85 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-RAUWOLSCINE -190 85 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-RAUWOLSCINE -190 85 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-RAUWOLSCINE -190 85 Human 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
2435 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
395 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
520 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5386 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
CHEMBL844 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
DB00484 7509 100 3H-Yohimbine -81 12 Pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 None
5280805 92180 81 None -28 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
Drug Central 610 6 10 16 -1.7 C[C@@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(-c4ccc(O)c(O)c4)oc4cc(O)cc(O)c4c3=O)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@H](O)[C@H]1O None
CHEMBL226335 92180 81 None -28 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to adrenergic alpha2A receptorBinding affinity to adrenergic alpha2A receptor
Drug Central 610 6 10 16 -1.7 C[C@@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(-c4ccc(O)c(O)c4)oc4cc(O)cc(O)c4c3=O)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@H](O)[C@H]1O None
1210 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 7705 51 None -416 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
3823 56995 42 None -40 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 56995 42 None -40 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 56995 42 None -40 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
28417 46813 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 46813 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
3652 53018 70 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 53018 70 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
135 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-RAUWOLSCINE -4 56 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1960 9632 67 None -35 26 Mouse 8.3 pKi = 8.3 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 9632 67 None -35 26 Mouse 8.3 pKi = 8.3 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 9632 67 None -35 26 Mouse 8.3 pKi = 8.3 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 9632 67 None -35 26 Mouse 8.3 pKi = 8.3 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 9632 67 None -35 26 Mouse 8.3 pKi = 8.3 Binding
Binding affinity to mouse alpha-2A receptor expressed in COS7 cellsBinding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
4158 212120 21 None -2 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 212120 21 None -2 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 212120 21 None -2 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
448537 167029 89 None -33 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 167029 89 None -33 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2812 11551 101 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
2719 7704 74 None -4 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 7704 74 None -4 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 7704 74 None -4 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 7704 74 None -4 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 7704 74 None -4 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscineActivity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
10836 21239 14 None -2 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 21239 14 None -2 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
4209 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 None -794 33 Pig 8.3 pKi = 8.3 Binding
Compound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]-RX 821002 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
6040 222812 0 3H-RAUWOLSCINE -4 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 233 2 0 3 2.3 C1CCN(CC1)CC2COC3=CC=CC=C3O2 None
2337 10030 77 None -50 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -50 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -50 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -50 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -50 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5268 10428 40 3H-RAUWOLSCINE -63 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-RAUWOLSCINE -63 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-RAUWOLSCINE -63 18 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
4211 64596 83 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
CHEMBL1670 64596 83 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
1443 8809 34 None -23 11 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 8809 34 None -23 11 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 8809 34 None -23 11 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 8809 34 None -23 11 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 8809 34 None -23 11 Human 8.3 pKi = 8.3 Binding
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
1549008 212459 85 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 None
CHEMBL822 212459 85 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 291 4 0 1 4.9 CN(C/C=C/C#CC(C)(C)C)Cc1cccc2ccccc12 None
121850 7513 0 3H-MK912 41 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 None
525 7513 0 3H-MK912 41 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 None
CHEMBL216097 7513 0 3H-MK912 41 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 None
3598 194600 76 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
CHEMBL496 194600 76 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
2402 10143 62 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
2247 7293 81 None -58 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 None -58 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 None -58 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 None -58 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 None -58 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
5198 26205 54 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 None
CHEMBL12948 26205 54 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 247 4 1 3 2.5 CC1CCC(NC(=O)N(CCCl)N=O)CC1 None
3117 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4209 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 None -263 33 Rat 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.The compound was tested for binding affinity against alpha-2d-adrenoceptor, from rat clones.
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
3198 212292 76 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 212292 76 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 212292 76 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
16362 9899 71 None -501 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 None -501 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 None -501 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 None -501 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 None -501 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
5318 22348 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 22348 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 22348 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
5353853 24758 47 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 24758 47 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 24758 47 None -16 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1836 9370 59 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 9370 59 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 9370 59 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 9370 59 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 9370 59 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
4189 213701 96 None -18 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 213701 96 None -18 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 213701 96 None -18 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2406 107180 89 None -16 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
CHEMBL290106 107180 89 None -16 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
119584 9373 102 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
1848 9373 102 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
242 9373 102 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
CHEMBL60889 9373 102 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
DB11675 9373 102 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
2484 215072 71 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 None
CHEMBL990 215072 71 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 317 4 0 1 5.8 CN(Cc1ccc(C(C)(C)C)cc1)Cc1cccc2ccccc12 None
2342 7386 39 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
331 7386 39 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
7124 7386 39 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
CHEMBL1201250 7386 39 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
DB00767 7386 39 None -1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
2335 18620 22 None -5 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 18620 22 None -5 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 18620 22 None -5 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 18620 22 None -5 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
1227 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 9267 43 None -91 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3168 16034 92 None -123 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 None -123 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1353 8692 93 None -190 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -190 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -190 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -190 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -190 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1830 9368 44 None -14 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 None -14 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 None -14 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 None -14 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 None -14 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3151 8244 97 None -99 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 8244 97 None -99 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 8244 97 None -99 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 8244 97 None -99 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 8244 97 None -99 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
1782 9296 84 None -5 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 9296 84 None -5 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 9296 84 None -5 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 9296 84 None -5 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 9296 84 None -5 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
135398737 7745 93 3H-RAUWOLSCINE -26 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-RAUWOLSCINE -26 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-RAUWOLSCINE -26 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-RAUWOLSCINE -26 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-RAUWOLSCINE -26 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2803 7742 58 3H-MK912 -1 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 3H-MK912 -1 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 3H-MK912 -1 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 3H-MK912 -1 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 3H-MK912 -1 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2105 9828 37 3H-RX821002 -13 32 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-RX821002 -13 32 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-RX821002 -13 32 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-RX821002 -13 32 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-RX821002 -13 32 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1343 8670 62 3H-MK912 -11 9 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 8670 62 3H-MK912 -11 9 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 8670 62 3H-MK912 -11 9 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 8670 62 3H-MK912 -11 9 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 8670 62 3H-MK912 -11 9 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
15897 9637 0 3H-CLONIDINE -134 36 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-CLONIDINE -134 36 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-CLONIDINE -134 36 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
11957583 222973 0 3H-Yohimbine - 1 Pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 391 1 2 3 3.4 C1CN=C(N1)NC2=C(C=C(C=C2Cl)I)Cl.Cl None
2398 7741 62 3H-RX821002 -14 29 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 7741 62 3H-RX821002 -14 29 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 7741 62 3H-RX821002 -14 29 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 7741 62 3H-RX821002 -14 29 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 7741 62 3H-RX821002 -14 29 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
6852400 222716 0 3H-RAUWOLSCINE -131 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-RAUWOLSCINE -131 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
3337 213146 27 3H-CLONIDINE -27 40 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-CLONIDINE -27 40 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-CLONIDINE -27 40 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-CLONIDINE -27 40 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-CLONIDINE -27 40 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
5268 10428 40 3H-MK912 -63 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-MK912 -63 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-MK912 -63 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
2726 7706 68 3H-RAUWOLSCINE -87 72 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-RAUWOLSCINE -87 72 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-RAUWOLSCINE -87 72 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-RAUWOLSCINE -87 72 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-RAUWOLSCINE -87 72 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
4158 212120 21 125I-Clonidine -2 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 212120 21 125I-Clonidine -2 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 212120 21 125I-Clonidine -2 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
484 9633 51 3H-Yohimbine -14 35 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-Yohimbine -14 35 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-Yohimbine -14 35 Pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
3952 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 8669 38 3H-Yohimbine -9 12 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
1222 8445 49 3H-RAUWOLSCINE -100 32 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 3H-RAUWOLSCINE -100 32 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 3H-RAUWOLSCINE -100 32 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 3H-RAUWOLSCINE -100 32 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 3H-RAUWOLSCINE -100 32 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
523 10878 93 35S-GTPGammaS -2 5 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
5707 10878 93 35S-GTPGammaS -2 5 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
CHEMBL297362 10878 93 35S-GTPGammaS -2 5 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
DB11477 10878 93 35S-GTPGammaS -2 5 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C None
2142 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-RAUWOLSCINE -2 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
6018 17837 96 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 None
CHEMBL117785 17837 96 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 None
463 8187 22 None -67 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
6918097 8187 22 None -67 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
837 8187 22 None -67 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
CHEMBL2051956 8187 22 None -67 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
DB14068 8187 22 None -67 13 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 609 10 1 8 6.0 COC(=O)C1=C(C)NC(=C([C@@H]1c1cccc(c1)[N+](=O)[O-])C(=O)OCCCN1CCC(CC1)(c1ccccc1)c1ccccc1)C None
237 211644 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL546257 211644 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL554190 211644 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 211644 48 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
2181 9902 46 None -58 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 None -58 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 None -58 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 None -58 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 None -58 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
1530 8963 50 None -70 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 8963 50 None -70 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 8963 50 None -70 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 8963 50 None -70 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 8963 50 None -70 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
4601 213526 35 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 213526 35 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 213526 35 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
5467 212707 43 None -6 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 212707 43 None -6 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
1577 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 None -3 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
657255 205863 34 None -10 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 205863 34 None -10 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
3157 8252 71 None -61 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 8252 71 None -61 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 8252 71 None -61 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 8252 71 None -61 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 8252 71 None -61 12 Human 8.2 pKi = 8.2 Binding
Binding affinity against Alpha-2A adrenergic receptor, from human clones.Binding affinity against Alpha-2A adrenergic receptor, from human clones.
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
1016 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 10519 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
4011 89183 49 None -35 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 89183 49 None -35 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
26757 214757 31 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 None
CHEMBL972 214757 31 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 187 4 0 1 2.2 C#CCN(C)[C@H](C)Cc1ccccc1 None
219050 10146 25 3H-RX821002 -38 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 10146 25 3H-RX821002 -38 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 10146 25 3H-RX821002 -38 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
240 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
214 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 None -75 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
209 9831 97 None -100 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 None -100 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 None -100 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 None -100 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 None -100 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2435 10362 83 None -123 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -123 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -123 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -123 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -123 48 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1042 8362 23 None -97 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 8362 23 None -97 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 8362 23 None -97 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 8362 23 None -97 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 8362 23 None -97 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2726 7706 68 None -87 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -87 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -87 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -87 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -87 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
134 9292 24 None -74 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 None -74 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 None -74 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 None -74 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 None -74 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2351 10059 64 None -9 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 10059 64 None -9 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 10059 64 None -9 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 10059 64 None -9 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 10059 64 None -9 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
150 9287 21 None -45 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 9287 21 None -45 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 9287 21 None -45 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 9287 21 None -45 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 9287 21 None -45 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
6726 8063 51 None -10 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 8063 51 None -10 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 8063 51 None -10 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 8063 51 None -10 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 8063 51 None -10 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
1222 8445 49 None -100 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 None -100 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 None -100 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 None -100 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 None -100 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
6075 156887 42 None -11 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 156887 42 None -11 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
3584 10549 64 None -251 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
5401 10549 64 None -251 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
7302 10549 64 None -251 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
CHEMBL611 10549 64 None -251 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
DB01162 10549 64 None -251 14 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 None
2398 7741 62 None -14 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 7741 62 None -14 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 7741 62 None -14 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 7741 62 None -14 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 7741 62 None -14 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
66265 100788 15 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 100788 15 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
4735 201894 96 None -9 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL361506 201894 96 None -9 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
CHEMBL55 201894 96 None -9 10 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 None
1225 8253 26 None -22 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 8253 26 None -22 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 8253 26 None -22 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 8253 26 None -22 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 8253 26 None -22 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2865 10915 73 None -64 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 None -64 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 None -64 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 None -64 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 None -64 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
41 8440 0 3H-RX821002 -5 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-RX821002 -5 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-RX821002 -5 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
2142 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 3H-PRAZOSIN -2 37 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
102 10899 48 3H-RX821002 -5 49 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-RX821002 -5 49 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-RX821002 -5 49 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-RX821002 -5 49 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-RX821002 -5 49 Human 8.2 pKi = 8.2 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
191 7191 98 None -41 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 None -41 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 None -41 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 None -41 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 None -41 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
3561 25849 39 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 25849 39 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
4098 39279 30 None -13 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 39279 30 None -13 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 39279 30 None -13 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
164512323 222810 0 3H-RAUWOLSCINE -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RAUWOLSCINE -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
441383 27105 57 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 27105 57 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
1548955 95356 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 95356 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 95356 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
135398745 9688 112 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1212 8443 50 None -165 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -165 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -165 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -165 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -165 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 224490 0 None -1 26 Human 8.2 pKi = 8.2 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
46780481 114308 20 3H-RAUWOLSCINE -47 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-RAUWOLSCINE -47 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-RAUWOLSCINE -47 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-RAUWOLSCINE -47 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3191 109635 97 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 109635 97 None -8 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
1028 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 None -48 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1971 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 9641 38 None -8 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
162265 209053 22 None -12 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 None -12 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 None -12 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
213 10625 55 None -10 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 None -10 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 None -10 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 None -10 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 None -10 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2286 9957 51 None -13 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 9957 51 None -13 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 9957 51 None -13 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 9957 51 None -13 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 9957 51 None -13 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2695 10613 81 None -9 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
5504 10613 81 None -9 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
7310 10613 81 None -9 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
CHEMBL770 10613 81 None -9 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
DB00797 10613 81 None -9 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 None
2162 48288 100 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
CHEMBL1491 48288 100 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
12488 8438 56 None -6 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 8438 56 None -6 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 8438 56 None -6 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 8438 56 None -6 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2520 210787 70 None -6 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL1280 210787 70 None -6 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL6966 210787 70 None -6 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
4209 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 None -1380 33 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptorAbility to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1201549 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 7384 24 None -33 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
103 10925 61 None -54 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -54 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -54 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -54 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -54 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
11057 182928 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 182928 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 182928 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 182928 23 None -1 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
1547484 7727 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 7727 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 7727 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 7727 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 7727 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3294 8787 111 None -47 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None -47 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None -47 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None -47 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None -47 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
12574 9383 88 None -33 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
4810 9383 88 None -33 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
CHEMBL19236 9383 88 None -33 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
DB09242 9383 88 None -33 6 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC None
1613 9127 53 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
15387 52596 55 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
5472 212597 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
CHEMBL1717 212597 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
CHEMBL833 212597 75 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 None
100 10577 58 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
180 7189 56 None -58 40 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 None -58 40 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 None -58 40 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 None -58 40 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 None -58 40 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2284 9956 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 9956 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 9956 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 9956 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 9956 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
228 7233 28 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
104870 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
68617 212306 62 None -3 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 212306 62 None -3 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 212306 62 None -3 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
4209 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 None -74 33 Bovine 8.2 pKi = 8.2 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
277 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 None -33 50 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
15897 9637 0 3H-CLONIDINE -134 36 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-CLONIDINE -134 36 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-CLONIDINE -134 36 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2803 7742 58 35S-GTPGammaS -1 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2803 7742 58 35S-GTPGammaS -3 19 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 35S-GTPGammaS -1 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 35S-GTPGammaS -3 19 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 35S-GTPGammaS -1 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 35S-GTPGammaS -3 19 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 35S-GTPGammaS -1 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 35S-GTPGammaS -3 19 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 35S-GTPGammaS -1 19 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 35S-GTPGammaS -3 19 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
102 10899 48 35S-GTPGammaS -154 49 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 35S-GTPGammaS -154 49 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 35S-GTPGammaS -154 49 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 35S-GTPGammaS -154 49 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 35S-GTPGammaS -154 49 Mouse 7.2 pKi = 7.2 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
2683 10606 60 3H-RAUWOLSCINE -3 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
5487 10606 60 3H-RAUWOLSCINE -3 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
7308 10606 60 3H-RAUWOLSCINE -3 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
CHEMBL1079 10606 60 3H-RAUWOLSCINE -3 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
DB00697 10606 60 3H-RAUWOLSCINE -3 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 None
102 10899 48 3H-PRAZOSIN -158 49 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-PRAZOSIN -158 49 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-PRAZOSIN -158 49 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-PRAZOSIN -158 49 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-PRAZOSIN -158 49 Rat 7.2 pKi = 7.2 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
2726 7706 68 3H-RX821002 -38 72 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-RX821002 -38 72 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-RX821002 -38 72 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-RX821002 -38 72 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-RX821002 -38 72 Pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2435 10362 83 3H-CLONIDINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 10362 83 3H-RAUWOLSCINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-CLONIDINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-RAUWOLSCINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-CLONIDINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-RAUWOLSCINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-CLONIDINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-RAUWOLSCINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-CLONIDINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-RAUWOLSCINE -123 48 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1028 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 7079 71 3H-Yohimbine -120 30 Pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
214 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-CLONIDINE -75 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 223104 0 3H-CLONIDINE -8 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
2202 9906 96 None -1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 None -1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 None -1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 None -1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 None -1 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
212 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 10578 47 None -6 25 Human 8.2 pKi = 8.2 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
242 7258 124 None -26 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -26 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -26 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -26 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -26 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
135398737 7745 93 None -26 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -26 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -26 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -26 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -26 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
26987 7736 33 None -158 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 7736 33 None -158 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 7736 33 None -158 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 7736 33 None -158 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 7736 33 None -158 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
1960 9632 67 None -23 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 9632 67 None -23 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 9632 67 None -23 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 9632 67 None -23 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 9632 67 None -23 26 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Alpha-2A adrenergic receptorBinding affinity for human Alpha-2A adrenergic receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
2274 9947 58 None -10 31 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -10 31 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -10 31 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -10 31 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -10 31 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
124 9755 47 35S-GTPGammaS -4 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 35S-GTPGammaS -4 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 35S-GTPGammaS -4 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 35S-GTPGammaS -4 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 35S-GTPGammaS -4 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2105 9828 37 None -13 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 None -13 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 None -13 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 None -13 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 None -13 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
117590588 103299 35 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O None
14969 103299 35 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O None
CHEMBL262777 103299 35 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1447 13 19 25 0.1 CN[C@H](CC(C)C)C(=O)N[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]2C(=O)N[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c4cc(O)cc(O)c4-c4cc3ccc4O)[C@H](O)c3ccc(c(Cl)c3)Oc3cc2cc(c3O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O[C@H]2C[C@](C)(N)[C@H](O)[C@H](C)O2)Oc2ccc(cc2Cl)[C@H]1O None
102 10899 48 None -47 49 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -47 49 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -47 49 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -47 49 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -47 49 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 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
213046 9164 59 None -19 9 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 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 None
4168 9164 59 None -19 9 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 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 None
7461 9164 59 None -19 9 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 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 None
CHEMBL1237021 9164 59 None -19 9 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 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 None
DB08815 9164 59 None -19 9 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 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 None
2585 7590 103 None -28 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 None -28 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 None -28 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 None -28 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 None -28 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
68712 107114 60 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
Drug Central 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
CHEMBL289480 107114 60 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
Drug Central 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
5524 223243 0 None 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 215 1 2 3 1.9 C1CCC2=C(C1)C=CC=C2NC3=NCCN3 None
240 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 7731 43 None -3 25 Rat 8.1 pKi = 8.1 Binding
Compound was evaluated for the binding affinity at Alpha adrenergic receptorCompound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2389 10104 118 None -37 66 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -37 66 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -37 66 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -37 66 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -37 66 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
6761 74574 19 None -6 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 74574 19 None -6 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
133 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
124 9755 47 None -16 32 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 None -16 32 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 None -16 32 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 None -16 32 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 None -16 32 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
11079 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
3369 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
4436 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
5509 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
CHEMBL761 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
DB06711 9510 63 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 None
1816 9318 102 None -51 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 9318 102 None -51 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 9318 102 None -51 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 9318 102 None -51 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 9318 102 None -51 18 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptorInhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
135398737 7745 93 None -10 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -10 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -10 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -10 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -10 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
931 223242 0 35S-GTPGammaS -2 4 Mouse 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 128 0 0 0 2.8 C1=CC=C2C=CC=CC2=C1 None
135 9310 43 None -5 56 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -5 56 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -5 56 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -5 56 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -5 56 Bovine 8.1 pKi = 8.1 Binding
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3952 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 8669 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
11978813 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
3658 10879 53 None -5 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 10879 53 None -5 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 10879 53 None -5 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 10879 53 None -5 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 10879 53 None -5 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
10219 195575 37 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 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 None
CHEMBL493439 195575 37 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 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 None
CHEMBL50588 195575 37 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 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 None
129211 10521 78 None -120 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
2562 10521 78 None -120 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
488 10521 78 None -120 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
CHEMBL836 10521 78 None -120 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
DB00706 10521 78 None -120 16 Human 8.1 pKi = 8.1 Binding
Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligandBinding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand
Drug Central 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C None
37 7565 60 None -3 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 7565 60 None -3 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 7565 60 None -3 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 7565 60 None -3 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 7565 60 None -3 17 Human 8.1 pKi = 8.1 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
115237 62359 119 None -44 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -44 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
2216 7234 50 35S-GTPGammaS 1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
229 7234 50 35S-GTPGammaS 1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
7117 7234 50 35S-GTPGammaS 1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
CHEMBL647 7234 50 35S-GTPGammaS 1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
DB00964 7234 50 35S-GTPGammaS 1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
41 8440 0 3H-MK912 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
41 8440 0 3H-RX821002 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-MK912 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-RX821002 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-MK912 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-RX821002 -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
102 10899 48 3H-MK912 -5 49 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-MK912 -5 49 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-MK912 -5 49 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-MK912 -5 49 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-MK912 -5 49 Human 8.1 pKi = 8.1 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
None 223108 0 3H-CLONIDINE 2 27 Human 6.1 pKi = 6.1 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
68712 107114 60 35S-GTPGammaS -9 5 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
CHEMBL289480 107114 60 35S-GTPGammaS -9 5 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 None
None 222914 0 3H-CLONIDINE -758 23 Human 6.1 pKi = 6.1 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
213 10625 55 125I-Clonidine -10 43 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 125I-Clonidine -10 43 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 125I-Clonidine -10 43 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 125I-Clonidine -10 43 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 125I-Clonidine -10 43 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
242 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-CLONIDINE -26 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
119570 9933 96 3H-CLONIDINE -41 39 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-CLONIDINE -41 39 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-CLONIDINE -41 39 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-CLONIDINE -41 39 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-CLONIDINE -41 39 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2726 7706 68 3H-RAUWOLSCINE -87 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-RAUWOLSCINE -87 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-RAUWOLSCINE -87 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-RAUWOLSCINE -87 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-RAUWOLSCINE -87 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 7745 93 3H-RAUWOLSCINE -26 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-RAUWOLSCINE -26 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-RAUWOLSCINE -26 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-RAUWOLSCINE -26 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-RAUWOLSCINE -26 90 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954259 222758 0 3H-CLONIDINE -263 43 Human 7.1 pKi = 7.1 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
4209 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 35S-GTPGammaS -1380 33 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
31101 7516 40 None -10 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 None -10 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 None -10 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 None -10 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 None -10 35 Human 8.1 pKi = 8.1 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
2389 10104 118 None -77 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -77 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -77 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -77 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -77 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
12575 8769 30 UNDEFINED -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 8769 30 UNDEFINED -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 8769 30 UNDEFINED -5 17 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
1209 8439 75 None -1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 8439 75 None -1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 8439 75 None -1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 8439 75 None -1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 8439 75 None -1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
5268 10428 40 3H-RAUWOLSCINE -63 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 3H-RAUWOLSCINE -63 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 3H-RAUWOLSCINE -63 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
135 9310 43 None -4 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -4 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -4 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -4 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -4 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2142 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 None -2 37 Rat 8.1 pKi = 8.1 Binding
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
102 10899 48 None -15 49 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -15 49 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -15 49 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -15 49 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -15 49 Pig 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-cloneCompound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug Central 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
1593 9119 66 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
30668 9119 66 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
9868 9119 66 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
CHEMBL17860 9119 66 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
DB04948 9119 66 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cellsDisplacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug Central 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl None
2803 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 None -1 19 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
134551 7146 27 None -3 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 7146 27 None -3 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 7146 27 None -3 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 7146 27 None -3 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2216 7234 50 None 1 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
229 7234 50 None 1 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
7117 7234 50 None 1 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
CHEMBL647 7234 50 None 1 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
DB00964 7234 50 None 1 6 Human 8.1 pKi = 8.1 Binding
Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cellsCompound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug Central 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 None
None 222814 0 3H-RAUWOLSCINE 1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 200 3 1 1 2.8 CC1=C(C(=CC=C1)C)CCC2=CN=CN2 None
2142 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 None -2 37 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]RX781094 from alpha2 adrenergic receptorDisplacement of [3H]RX781094 from alpha2 adrenergic receptor
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
124 9755 47 None -5 32 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 None -5 32 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 None -5 32 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 None -5 32 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 None -5 32 Bovine 8.1 pKi = 8.1 Binding
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pinealCompound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
164512323 222810 0 3H-RAUWOLSCINE -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
6419959 222810 0 3H-RAUWOLSCINE -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 352 1 1 4 3.2 CC1C2CN3CCC4=C(C3CC2C(=CO1)C(=O)OC)NC5=CC=CC=C45 None
11954259 222758 0 3H-CLONIDINE -263 43 Human 7.1 pKi = 7.1 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
3337 213146 27 3H-CLONIDINE -27 40 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-CLONIDINE -27 40 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-CLONIDINE -27 40 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-CLONIDINE -27 40 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-CLONIDINE -27 40 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
209 9831 97 3H-CLONIDINE -100 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 3H-CLONIDINE -100 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 3H-CLONIDINE -100 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 3H-CLONIDINE -100 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 3H-CLONIDINE -100 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2803 7742 58 3H-Yohimbine -5 19 Pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 3H-Yohimbine -5 19 Pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 3H-Yohimbine -5 19 Pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 3H-Yohimbine -5 19 Pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 3H-Yohimbine -5 19 Pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
11293787 154992 0 UNDEFINED -77 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 None
CHEMBL393597 154992 0 UNDEFINED -77 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 6 0 5 5.8 COc1cc2c(cc1OC)CN(Cc1ccc(OC)c3oc(-c4ccccc4F)cc13)CC2 None
2181 9902 46 3H-RAUWOLSCINE -58 34 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 3H-RAUWOLSCINE -58 34 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 3H-RAUWOLSCINE -58 34 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 3H-RAUWOLSCINE -58 34 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 3H-RAUWOLSCINE -58 34 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2202 9906 96 3H-RX821002 -1 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 3H-RX821002 -1 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 3H-RX821002 -1 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 3H-RX821002 -1 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 3H-RX821002 -1 21 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
None 223109 0 UNDEFINED -8 27 Human 8.1 pKi = 8.1 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
2142 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 None 1 37 Bovine 8.0 pKi = 8.0 Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligandBinding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
11954224 222732 0 None -446 59 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
107715 207724 22 None -6 20 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 207724 22 None -6 20 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 207724 22 None -6 20 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
931 223242 0 35S-GTPGammaS -2 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 128 0 0 0 2.8 C1=CC=C2C=CC=CC2=C1 None
102 10899 48 None -5 49 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -5 49 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -5 49 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -5 49 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -5 49 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligandBinding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
Drug Central 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
2803 7742 58 None 1 19 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 None 1 19 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 None 1 19 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 None 1 19 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 None 1 19 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards alpha-2D adrenergic receptorBinding affinity towards alpha-2D adrenergic receptor
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
10531 8202 21 None -5 24 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 8202 21 None -5 24 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 8202 21 None -5 24 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 8202 21 None -5 24 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 8202 21 None -5 24 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
2601 10552 33 None -1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 None -1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 None -1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 None -1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 None -1 21 Human 8.0 pKi = 8.0 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
124 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
124 9755 47 3H-MK912 -4 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-MK912 -4 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-MK912 -4 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-MK912 -4 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-MK912 -4 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
12575 8769 30 35S-GTPGammaS -5 17 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 8769 30 35S-GTPGammaS -5 17 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 8769 30 35S-GTPGammaS -5 17 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
1588 9105 27 None 1 44 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 None 1 44 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 None 1 44 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 None 1 44 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 None 1 44 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
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
1576 223105 0 3H-CLONIDINE -15 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
1343 8670 62 35S-GTPGammaS -11 9 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 8670 62 35S-GTPGammaS -11 9 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 8670 62 35S-GTPGammaS -11 9 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 8670 62 35S-GTPGammaS -11 9 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 8670 62 35S-GTPGammaS -11 9 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
None 223109 0 3H-CLONIDINE -8 27 Human 5.0 pKi = 5.0 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
21830793 98610 10 3H-8-OH-DPAT -630 46 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 98610 10 3H-8-OH-DPAT -630 46 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
None 222815 0 3H-RAUWOLSCINE -16 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 334 4 1 4 4.6 CN(C)CCCN1C2=C(C=C(C=C2)O)SC3=C1C=C(C=C3)Cl None
484 9633 51 3H-RAUWOLSCINE -9 35 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-RAUWOLSCINE -9 35 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-RAUWOLSCINE -9 35 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
1593 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
30668 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
9868 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
CHEMBL17860 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
DB04948 9119 66 None 5 4 Human 8.4 pKi = 8.4 Binding
Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2A</sub>-AR.
Guide to Pharmacology 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 22341244
1816 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 15771415
1816 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 35224877
4205 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 15771415
4205 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 35224877
7241 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 15771415
7241 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 35224877
CHEMBL654 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 15771415
CHEMBL654 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 35224877
DB00370 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 15771415
DB00370 9318 102 None -51 18 Human 7.0 pKi = 7.0 Binding
Inhibition of [<sup>3</sup>H]rauwolscine binding.Inhibition of [<sup>3</sup>H]rauwolscine binding.
Guide to Pharmacology 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 35224877
2695 10613 81 None -9 6 Human 6.7 pKi = 6.7 Binding
Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S bindingInhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding
Guide to Pharmacology 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 9605427
5504 10613 81 None -9 6 Human 6.7 pKi = 6.7 Binding
Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S bindingInhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding
Guide to Pharmacology 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 9605427
7310 10613 81 None -9 6 Human 6.7 pKi = 6.7 Binding
Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S bindingInhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding
Guide to Pharmacology 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 9605427
CHEMBL770 10613 81 None -9 6 Human 6.7 pKi = 6.7 Binding
Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S bindingInhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding
Guide to Pharmacology 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 9605427
DB00797 10613 81 None -9 6 Human 6.7 pKi = 6.7 Binding
Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S bindingInhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding
Guide to Pharmacology 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 9605427
174174 7311 49 None -43651 14 Human 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 29860464
260 7311 49 None -43651 14 Human 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 29860464
320 7311 49 None -43651 14 Human 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 29860464
CHEMBL517712 7311 49 None -43651 14 Human 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 29860464
DB00572 7311 49 None -43651 14 Human 4.9 pKi = 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 29860464
12574 9383 88 None -33 6 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
4810 9383 88 None -33 6 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
CHEMBL19236 9383 88 None -33 6 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
DB09242 9383 88 None -33 6 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 36101495
523 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
523 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
5707 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
5707 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
CHEMBL297362 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
CHEMBL297362 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
DB11477 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 36101495
DB11477 10878 93 None -2 5 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 220 1 1 3 3.2 Cc1cccc(c1NC1=NCCCS1)C 9605427
1960 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
1960 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
1960 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
439260 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
439260 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
439260 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
505 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
505 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
505 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
CHEMBL1437 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL1437 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL1437 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
DB00368 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00368 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00368 9632 67 None -23 26 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 9824686
1028 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
1028 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
1028 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
139148732 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
139148732 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
139148732 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
479 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
479 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
479 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
5816 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
5816 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
5816 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
CHEMBL679 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
CHEMBL679 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
CHEMBL679 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
DB00668 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 36101495
DB00668 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9605427
DB00668 7079 71 None -48 30 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9824686
4209 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
4209 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
4209 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
4893 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
4893 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
4893 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
503 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
503 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
503 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
5385 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
5385 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
5385 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
CHEMBL2 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
CHEMBL2 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
CHEMBL2 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
DB00457 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 1353247
DB00457 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 35224877
DB00457 9937 75 None -1380 33 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 7908642
2683 10606 60 None -3 4 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
5487 10606 60 None -3 4 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
7308 10606 60 None -3 4 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
CHEMBL1079 10606 60 None -3 4 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
DB00697 10606 60 None -3 4 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 36101495
2726 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
2726 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
2726 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
621 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
621 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
621 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
83 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
83 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
83 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
CHEMBL71 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
CHEMBL71 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
CHEMBL71 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
DB00477 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1353247
DB00477 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 35224877
DB00477 7706 68 None -87 72 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908642
122211 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 1353247
122211 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 35224877
122211 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7908642
524 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 1353247
524 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 35224877
524 7250 0 None -239 6 Human 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 5 0 5 3.6 COc1ccccc1N1CCN(CC1)CCC1C(=O)c2ccccc2C(C1=O)(C)C 7908642
1343 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
1343 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9283709
1343 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
3519 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
3519 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9283709
3519 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
522 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
522 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9283709
522 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
CHEMBL862 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
CHEMBL862 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9283709
CHEMBL862 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
DB01018 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 36101495
DB01018 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9283709
DB01018 8670 62 None -11 9 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 9605427
11079 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
3369 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
4436 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
5509 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
CHEMBL761 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
DB06711 9510 63 None -1 5 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 36101495
213046 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 20404009
213046 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
4168 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 20404009
4168 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
7461 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 20404009
7461 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
CHEMBL1237021 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 20404009
CHEMBL1237021 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
DB08815 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 20404009
DB08815 9164 59 None -19 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
5268 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
5268 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
53 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
53 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
CHEMBL300555 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 35224877
CHEMBL300555 10428 40 None -63 18 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 7996470
12575 8769 30 None -5 17 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 35224877
54459 8769 30 None -5 17 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 35224877
CHEMBL10316 8769 30 None -5 17 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 35224877
2389 10104 118 None -77 66 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 35224877
5073 10104 118 None -77 66 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 35224877
96 10104 118 None -77 66 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 35224877
CHEMBL85 10104 118 None -77 66 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 35224877
DB00734 10104 118 None -77 66 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 35224877
3952 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
3952 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5353646 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5353646 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5443 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5443 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
5702063 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
5702063 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
CHEMBL1331786 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL1331786 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
CHEMBL420 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 36101495
CHEMBL420 8669 38 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 9605427
13180 7550 0 None - 1 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 13 2 4 7.4 C(CCCCCNC1=C2C=CC=CC2=NC=C1)CCCCNC3=CC=NC4=C3C=CC=C4 32694911
151782 7550 0 None - 1 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 13 2 4 7.4 C(CCCCCNC1=C2C=CC=CC2=NC=C1)CCCCNC3=CC=NC4=C3C=CC=C4 32694911
CHEMBL121656 7550 0 None - 1 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 13 2 4 7.4 C(CCCCCNC1=C2C=CC=CC2=NC=C1)CCCCNC3=CC=NC4=C3C=CC=C4 32694911
2435 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
2435 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
2435 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
2435 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
2435 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
395 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
395 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
395 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
395 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
395 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
520 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
520 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
520 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
520 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
520 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
5386 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
5386 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
5386 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
5386 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
5386 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
CHEMBL844 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
CHEMBL844 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
CHEMBL844 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
CHEMBL844 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
CHEMBL844 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
DB00484 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 36101495
DB00484 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9227000
DB00484 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9605427
DB00484 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9760042
DB00484 7509 100 None -2 12 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 9824686
3658 10879 53 None -5 8 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
517 10879 53 None -5 8 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
5709 10879 53 None -5 8 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
CHEMBL312448 10879 53 None -5 8 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
DB06694 10879 53 None -5 8 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 36101495
2142 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
2142 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
2142 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
4920903 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
4920903 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
4920903 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
502 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
502 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
502 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
5775 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
5775 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
5775 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
CHEMBL597 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
CHEMBL597 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
CHEMBL597 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
DB00692 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 1353247
DB00692 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 35224877
DB00692 9870 58 None -2 37 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 7908642
2803 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
2803 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
2803 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
2803 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
516 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
516 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
516 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
516 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
704 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
704 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
704 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
704 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
CHEMBL134 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
CHEMBL134 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
CHEMBL134 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
CHEMBL134 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
DB00575 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 36101495
DB00575 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9605427
DB00575 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9760042
DB00575 7742 58 None -1 19 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 9824686
124 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
124 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
124 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9227000
124 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
2032 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
2032 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
2032 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9227000
2032 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
4636 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
4636 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
4636 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9227000
4636 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
CHEMBL762 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
CHEMBL762 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
CHEMBL762 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9227000
CHEMBL762 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
DB00935 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 36101495
DB00935 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 7996470
DB00935 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9227000
DB00935 9755 47 None -4 32 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9605427
121850 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 2573535
121850 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
121850 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
525 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 2573535
525 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
525 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
CHEMBL216097 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 2573535
CHEMBL216097 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 35224877
CHEMBL216097 7513 0 None 41 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 215 2 1 3 1.6 CC1N(CC2=NCCN2)Cc2c1cccc2 7996470
31101 7516 40 None -10 35 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
31101 7516 40 None -10 35 Human 8.2 pKi = 8.2 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 36101495
35 7516 40 None -10 35 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 7516 40 None -10 35 Human 8.2 pKi = 8.2 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 36101495
403 7516 40 None -10 35 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 7516 40 None -10 35 Human 8.2 pKi = 8.2 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 36101495
CHEMBL493 7516 40 None -10 35 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 7516 40 None -10 35 Human 8.2 pKi = 8.2 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 36101495
DB01200 7516 40 None -10 35 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 7516 40 None -10 35 Human 8.2 pKi = 8.2 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 36101495
499 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
499 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
499 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
5685 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
5685 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
5685 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
CHEMBL25554 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 1353247
CHEMBL25554 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 35224877
CHEMBL25554 10849 18 None -13 14 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 7908642
313 9468 0 None -2 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29860464
2216 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
229 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
7117 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
CHEMBL647 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
DB00964 7234 50 None 1 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 1 3 4 1.9 Nc1cc(Cl)c(c(c1)Cl)NC1=NCCN1 8784451
12576 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 35224877
71310 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 35224877
CHEMBL353972 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 35224877
DB11481 7302 94 None -2 6 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 2 1 1 2.9 CCC1(CC2=CC=CC=C2C1)C3=CN=CN3 35224877
521 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
521 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9227000
521 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
521 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
521 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
5311068 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
5311068 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9227000
5311068 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
5311068 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
5311068 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
835 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
835 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9227000
835 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
835 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
835 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
CHEMBL778 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
CHEMBL778 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9227000
CHEMBL778 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
CHEMBL778 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
CHEMBL778 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
DB00633 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 36101495
DB00633 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9227000
DB00633 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9605427
DB00633 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9760042
DB00633 8186 69 None -6 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C 9824686
108094 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
108094 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
526 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
526 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
528 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
528 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
CHEMBL10332 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 35224877
CHEMBL10332 10196 27 None -1 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 234 2 1 5 0.8 COC1(COc2c(O1)cccc2)C1=NCCN1 7996470
12577 9341 0 None -15 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 0 0 3 3.3 CN1CC[C@]2(CCN3CCC4=C([C@@H]3C2)OC5=CC=CC=C45)N(C1=O)C 35224877
189711 9341 0 None -15 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 0 0 3 3.3 CN1CC[C@]2(CCN3CCC4=C([C@@H]3C2)OC5=CC=CC=C45)N(C1=O)C 35224877
CHEMBL1257057 9341 0 None -15 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 0 0 3 3.3 CN1CC[C@]2(CCN3CCC4=C([C@@H]3C2)OC5=CC=CC=C45)N(C1=O)C 35224877
102 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
102 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
102 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7908642
102 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
3659 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
3659 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
3659 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7908642
3659 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
8969 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
8969 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
8969 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7908642
8969 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
CHEMBL15245 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
CHEMBL15245 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
CHEMBL15245 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7908642
CHEMBL15245 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
DB01392 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 1353247
DB01392 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 35224877
DB01392 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7908642
DB01392 10899 48 None -5 49 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
13128 10173 0 None -3 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 364 3 0 4 2.4 CCS(=O)(=O)N1CCC[C@H]2[C@@H]1C[C@H]3C4=C(CCN3C2)C=C(C=C4)OC 35224877
9908992 10173 0 None -3 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 364 3 0 4 2.4 CCS(=O)(=O)N1CCC[C@H]2[C@@H]1C[C@H]3C4=C(CCN3C2)C=C(C=C4)OC 35224877
CHEMBL4303564 10173 0 None -3 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 364 3 0 4 2.4 CCS(=O)(=O)N1CCC[C@H]2[C@@H]1C[C@H]3C4=C(CCN3C2)C=C(C=C4)OC 35224877
1588 9105 27 None 1 44 Human 9.7 pKi = 9.7 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
1588 9105 27 None 1 44 Human 9.7 pKi = 9.7 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 35224877
28864 9105 27 None 1 44 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 9105 27 None 1 44 Human 9.7 pKi = 9.7 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 35224877
43 9105 27 None 1 44 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 9105 27 None 1 44 Human 9.7 pKi = 9.7 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 35224877
CHEMBL157138 9105 27 None 1 44 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 9105 27 None 1 44 Human 9.7 pKi = 9.7 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 35224877
DB00589 9105 27 None 1 44 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 9105 27 None 1 44 Human 9.7 pKi = 9.7 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 35224877
2995 211184 53 None -12 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 None -12 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 None -12 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
179 7188 115 None -35 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 None -35 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 None -35 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 None -35 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 None -35 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
3337 213146 27 None -27 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 None -27 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 None -27 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 None -27 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 None -27 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
119570 9933 96 None -41 39 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 None -41 39 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 None -41 39 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 None -41 39 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 None -41 39 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
46780481 114308 20 None -47 53 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 None -47 53 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 None -47 53 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 None -47 53 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
228 7233 28 None -5 23 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 7233 28 None -5 23 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 7233 28 None -5 23 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 7233 28 None -5 23 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 7233 28 None -5 23 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
2202 9906 96 None -1 21 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 9906 96 None -1 21 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 9906 96 None -1 21 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 9906 96 None -1 21 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 9906 96 None -1 21 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
2105 9828 37 None -13 32 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 9828 37 None -13 32 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 9828 37 None -13 32 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 9828 37 None -13 32 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 9828 37 None -13 32 Human 7.3 pKi None 7.3 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
37 7565 60 None -3 17 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 7565 60 None -3 17 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 7565 60 None -3 17 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 7565 60 None -3 17 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 7565 60 None -3 17 Human 7.9 pKi None 7.9 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
136 10065 32 None -3 16 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
223 10065 32 None -3 16 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
643606 10065 32 None -3 16 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
CHEMBL10347 10065 32 None -3 16 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7996470
2601 10552 33 None -1 21 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
443951 10552 33 None -1 21 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
56 10552 33 None -1 21 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
CHEMBL73151 10552 33 None -1 21 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666
DB13399 10552 33 None -1 21 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 12388666